LIPE

UniProt ID: Q05469
Organism: Homo sapiens
Review Status: COMPLETE
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Gene Description

LIPE encodes hormone-sensitive lipase (HSL), an intracellular neutral-lipid serine hydrolase that is recruited from the cytosol to lipid droplets during stimulated lipolysis. Its best-supported core catalytic role is hydrolysis of diacylglycerol to monoacylglycerol and fatty acid in the adipocyte lipolysis cascade; it also hydrolyzes other neutral esters, including triacylglycerols, cholesteryl esters, monoacylglycerols, and retinyl esters in tissue-specific contexts.

Existing Annotations Review

GO Term Evidence Action Reason
GO:0004771 sterol ester esterase activity
IBA
GO_REF:0000033
KEEP AS NON CORE
Summary: Sterol ester esterase activity is supported as a secondary neutral-ester substrate activity rather than the central adipocyte DAG-lipase role.
Reason: sterol ester esterase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
PMID:15716583
Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for adrenal steroidogenesis.
GO:0004806 triacylglycerol lipase activity
IBA
GO_REF:0000033
KEEP AS NON CORE
Summary: Triacylglycerol lipase activity is biochemically supported, but HSL is positioned primarily as the DAG lipase downstream of ATGL in stimulated lipolysis.
Reason: triacylglycerol lipase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
GO:0005829 cytosol
IBA
GO_REF:0000033
ACCEPT
Summary: The cytosol annotation is consistent with basal HSL localization before stimulated lipid-droplet recruitment.
Reason: cytosol is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0019433 triglyceride catabolic process
IBA
GO_REF:0000033
ACCEPT
Summary: HSL acts within the canonical triglyceride catabolic cascade by hydrolyzing DAG produced from TAG.
Reason: triglyceride catabolic process is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
GO:0042572 retinol metabolic process
IEA
GO_REF:0000120
KEEP AS NON CORE
Summary: Retinol metabolism is supported by recent physiology but is a tissue/context-specific secondary role rather than the primary neutral-lipid lipolysis function.
Reason: retinol metabolic process is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In 2024, adipocyte HSL was shown to be required for maintenance of circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A role.
GO:0004771 sterol ester esterase activity
IEA
GO_REF:0000117
KEEP AS NON CORE
Summary: Sterol ester esterase activity is supported as a secondary neutral-ester substrate activity rather than the central adipocyte DAG-lipase role.
Reason: sterol ester esterase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
PMID:15716583
Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for adrenal steroidogenesis.
GO:0004806 triacylglycerol lipase activity
IEA
GO_REF:0000120
KEEP AS NON CORE
Summary: Triacylglycerol lipase activity is biochemically supported, but HSL is positioned primarily as the DAG lipase downstream of ATGL in stimulated lipolysis.
Reason: triacylglycerol lipase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
GO:0005811 lipid droplet
IEA
GO_REF:0000044
ACCEPT
Summary: The lipid droplet annotation captures the regulated site where HSL gains access to stored neutral lipid substrates.
Reason: lipid droplet is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0005829 cytosol
IEA
GO_REF:0000044
ACCEPT
Summary: The cytosol annotation is consistent with basal HSL localization before stimulated lipid-droplet recruitment.
Reason: cytosol is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0005886 plasma membrane
IEA
GO_REF:0000044
KEEP AS NON CORE
Summary: Plasma membrane association has experimental support through PTRF/caveola studies, but it is not the main functional location of HSL.
Reason: plasma membrane is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
PMID:17026959
In the plasma membrane PTRF was specifically bound to a triacylglycerol-metabolizing subclass of caveolae containing hormone-sensitive lipase (HSL).
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0005901 caveola
IEA
GO_REF:0000044
KEEP AS NON CORE
Summary: Caveola association is supported in adipocytes through PTRF, but it is secondary to cytosol-to-lipid-droplet recruitment during lipolysis.
Reason: caveola is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
PMID:17026959
In the plasma membrane PTRF was specifically bound to a triacylglycerol-metabolizing subclass of caveolae containing hormone-sensitive lipase (HSL).
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0006629 lipid metabolic process
IEA
GO_REF:0000043
MODIFY
Summary: The generic lipid metabolic process annotation is directionally correct but too broad for HSL. Lipid catabolic process, and more specifically diacylglycerol catabolic process, better capture the reviewed function.
Reason: lipid metabolic process is less informative than the reviewed LIPE/HSL lipolysis term.
Proposed replacements: lipid catabolic process
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0008202 steroid metabolic process
IEA
GO_REF:0000043
KEEP AS NON CORE
Summary: Steroid metabolic process is plausible through cholesteryl ester hydrolysis in steroidogenic tissues but is not the central LIPE function.
Reason: steroid metabolic process is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
PMID:15716583
Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for adrenal steroidogenesis.
GO:0008203 cholesterol metabolic process
IEA
GO_REF:0000120
KEEP AS NON CORE
Summary: Cholesterol metabolism is supported through cholesteryl ester hydrolysis, but this is a secondary substrate context.
Reason: cholesterol metabolic process is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
PMID:15716583
The relatively higher turnover of HSL on CO observed in vitro adds further molecular insight on the physiological importance of HSL in cholesteryl ester catabolism in vivo.
GO:0016042 lipid catabolic process
IEA
GO_REF:0000120
ACCEPT
Summary: Lipid catabolic process is supported because LIPE/HSL hydrolyzes neutral lipid esters during lipolysis.
Reason: lipid catabolic process is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0016298 lipase activity
IEA
GO_REF:0000002
MODIFY
Summary: Generic lipase activity should be refined to diacylglycerol lipase activity because DAG hydrolysis is the best-supported core catalytic step.
Reason: lipase activity is less informative than the reviewed LIPE/HSL lipolysis term.
Proposed replacements: diacylglycerol lipase activity
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0016787 hydrolase activity
IEA
GO_REF:0000120
MODIFY
Summary: Generic hydrolase activity obscures the specific serine-lipase reaction supported for LIPE/HSL.
Reason: hydrolase activity is less informative than the reviewed LIPE/HSL lipolysis term.
Proposed replacements: diacylglycerol lipase activity
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0047372 monoacylglycerol lipase activity
IEA
GO_REF:0000120
KEEP AS NON CORE
Summary: Monoacylglycerol lipase activity is consistent with broad HSL substrate specificity, but the dominant physiological lipolysis role is DAG hydrolysis.
Reason: monoacylglycerol lipase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0047376 all-trans-retinyl-palmitate hydrolase, all-trans-retinol forming activity
IEA
GO_REF:0000116
KEEP AS NON CORE
Summary: Retinyl-palmitate hydrolase activity is supported as part of retinoid mobilization but should be treated as a secondary substrate-specific function.
Reason: all-trans-retinyl-palmitate hydrolase, all-trans-retinol forming activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In 2024, adipocyte HSL was shown to be required for maintenance of circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A role.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0050253 retinyl-palmitate esterase activity
IEA
GO_REF:0000117
KEEP AS NON CORE
Summary: Retinyl-palmitate esterase activity is supported as part of retinoid mobilization but is secondary to the primary DAG lipase role.
Reason: retinyl-palmitate esterase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In 2024, adipocyte HSL was shown to be required for maintenance of circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A role.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0120516 diacylglycerol lipase activity
IEA
GO_REF:0000120
ACCEPT
Summary: Diacylglycerol lipase activity is the best-supported core molecular function of HSL.
Reason: diacylglycerol lipase activity is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0005515 protein binding
IPI
PMID:32296183
A reference map of the human binary protein interactome.
MARK AS OVER ANNOTATED
Summary: Protein binding is too generic for curation of LIPE; the reviewed biology is better represented by regulated localization to PLIN1-coated lipid droplets and specific lipid hydrolase activities.
Reason: protein binding overstates or obscures the specific supported LIPE function.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0005829 cytosol
IDA
GO_REF:0000052
ACCEPT
Summary: The cytosol annotation is consistent with basal HSL localization before stimulated lipid-droplet recruitment.
Reason: cytosol is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0019433 triglyceride catabolic process
IEA
GO_REF:0000041
ACCEPT
Summary: HSL acts within the canonical triglyceride catabolic cascade by hydrolyzing DAG produced from TAG.
Reason: triglyceride catabolic process is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
GO:0004771 sterol ester esterase activity
IDA
PMID:15716583
Continuous monitoring of cholesterol oleate hydrolysis by ho...
KEEP AS NON CORE
Summary: Sterol ester esterase activity is supported as a secondary neutral-ester substrate activity rather than the central adipocyte DAG-lipase role.
Reason: sterol ester esterase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
PMID:15716583
Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for adrenal steroidogenesis.
GO:0004771 sterol ester esterase activity
IDA
PMID:8812477
Molecular cloning, genomic organization, and expression of a...
KEEP AS NON CORE
Summary: Sterol ester esterase activity is supported as a secondary neutral-ester substrate activity rather than the central adipocyte DAG-lipase role.
Reason: sterol ester esterase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
PMID:15716583
Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for adrenal steroidogenesis.
GO:0004806 triacylglycerol lipase activity
IDA
PMID:15716583
Continuous monitoring of cholesterol oleate hydrolysis by ho...
KEEP AS NON CORE
Summary: Triacylglycerol lipase activity is biochemically supported, but HSL is positioned primarily as the DAG lipase downstream of ATGL in stimulated lipolysis.
Reason: triacylglycerol lipase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
GO:0004806 triacylglycerol lipase activity
IDA
PMID:15955102
Identification of a novel keratinocyte retinyl ester hydrola...
KEEP AS NON CORE
Summary: Triacylglycerol lipase activity is biochemically supported, but HSL is positioned primarily as the DAG lipase downstream of ATGL in stimulated lipolysis.
Reason: triacylglycerol lipase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
GO:0016020 membrane
ISS
GO_REF:0000024
KEEP AS NON CORE
Summary: Generic membrane association is retained as non-core because HSL can associate with caveolae and lipid droplets while remaining primarily a regulated soluble lipase.
Reason: membrane is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
PMID:17026959
In the plasma membrane PTRF was specifically bound to a triacylglycerol-metabolizing subclass of caveolae containing hormone-sensitive lipase (HSL).
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0046340 diacylglycerol catabolic process
ISS
GO_REF:0000024
ACCEPT
Summary: Diacylglycerol catabolic process is the most precise biological-process annotation for HSL in the lipolysis cascade.
Reason: diacylglycerol catabolic process is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
GO:0046485 ether lipid metabolic process
ISS
GO_REF:0000024
MARK AS OVER ANNOTATED
Summary: Ether lipid metabolic process is not supported by the reviewed LIPE literature; the evidence supports neutral acylglycerol, sterol ester, and retinyl ester hydrolysis instead.
Reason: ether lipid metabolic process overstates or obscures the specific supported LIPE function.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0047372 monoacylglycerol lipase activity
ISS
GO_REF:0000024
KEEP AS NON CORE
Summary: Monoacylglycerol lipase activity is consistent with broad HSL substrate specificity, but the dominant physiological lipolysis role is DAG hydrolysis.
Reason: monoacylglycerol lipase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0050253 retinyl-palmitate esterase activity
IDA
PMID:15955102
Identification of a novel keratinocyte retinyl ester hydrola...
KEEP AS NON CORE
Summary: Retinyl-palmitate esterase activity is supported as part of retinoid mobilization but is secondary to the primary DAG lipase role.
Reason: retinyl-palmitate esterase activity is supported, but it is secondary to the core DAG-lipase role.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In 2024, adipocyte HSL was shown to be required for maintenance of circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A role.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0120516 diacylglycerol lipase activity
ISS
GO_REF:0000024
ACCEPT
Summary: Diacylglycerol lipase activity is the best-supported core molecular function of HSL.
Reason: diacylglycerol lipase activity is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0120516 diacylglycerol lipase activity
IDA
PMID:19800417
In vitro stereoselective hydrolysis of diacylglycerols by ho...
ACCEPT
Summary: Diacylglycerol lipase activity is the best-supported core molecular function of HSL.
Reason: diacylglycerol lipase activity is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0120516 diacylglycerol lipase activity
IDA
PMID:8812477
Molecular cloning, genomic organization, and expression of a...
ACCEPT
Summary: Diacylglycerol lipase activity is the best-supported core molecular function of HSL.
Reason: diacylglycerol lipase activity is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0005811 lipid droplet
ISS
GO_REF:0000024
ACCEPT
Summary: The lipid droplet annotation captures the regulated site where HSL gains access to stored neutral lipid substrates.
Reason: lipid droplet is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0016042 lipid catabolic process
ISS
GO_REF:0000024
ACCEPT
Summary: Lipid catabolic process is supported because LIPE/HSL hydrolyzes neutral lipid esters during lipolysis.
Reason: lipid catabolic process is supported as part of LIPE/HSL core lipid-droplet lipolysis.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
file:human/LIPE/LIPE-deep-research-falcon.md
HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
GO:0005515 protein binding
IPI
PMID:17026959
Association and insulin regulated translocation of hormone-s...
MARK AS OVER ANNOTATED
Summary: Protein binding is too generic for curation of LIPE; the reviewed biology is better represented by regulated localization to PLIN1-coated lipid droplets and specific lipid hydrolase activities.
Reason: protein binding overstates or obscures the specific supported LIPE function.
Supporting Evidence:
file:human/LIPE/LIPE-deep-research-falcon.md
HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
GO:0006468 protein phosphorylation
TAS
PMID:3420405
Hormone-sensitive lipase: sequence, expression, and chromoso...
REMOVE
Summary: This annotation treats LIPE as if it performs protein phosphorylation. The cited biology describes HSL as a phosphorylation-regulated lipase, not a kinase.
Reason: LIPE is regulated by phosphorylation but does not catalyze protein phosphorylation.
Supporting Evidence:
PMID:3420405
Hormone-sensitive lipase, a key enzyme in fatty acid mobilization, overall energy homeostasis, and possibly steroidogenesis, is acutely controlled through reversible phosphorylation by catecholamines and insulin.

Core Functions

Cytosol-to-lipid-droplet diacylglycerol lipase activity during hormonally stimulated neutral-lipid mobilization.

Supporting Evidence:
  • file:human/LIPE/LIPE-deep-research-falcon.md
    In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is further hydrolyzed by **MAGL** to glycerol and fatty acids.
  • file:human/LIPE/LIPE-deep-research-falcon.md
    HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access.
  • file:human/LIPE/LIPE-deep-research-falcon.md
    HSL has **broad substrate specificity**, with reported activity against **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.

References

Gene Ontology annotation through association of InterPro records with GO terms
Manual transfer of experimentally-verified manual GO annotation data to orthologs by curator judgment of sequence similarity
Annotation inferences using phylogenetic trees
Gene Ontology annotation based on UniPathway vocabulary mapping
Gene Ontology annotation based on UniProtKB/Swiss-Prot keyword mapping
Gene Ontology annotation based on UniProtKB/Swiss-Prot Subcellular Location vocabulary mapping, accompanied by conservative changes to GO terms applied by UniProt
Gene Ontology annotation based on curation of immunofluorescence data
Automatic Gene Ontology annotation based on Rhea mapping
Electronic Gene Ontology annotations created by ARBA machine learning models
Combined Automated Annotation using Multiple IEA Methods
Continuous monitoring of cholesterol oleate hydrolysis by hormone-sensitive lipase and other cholesterol esterases.
Identification of a novel keratinocyte retinyl ester hydrolase as a transacylase and lipase.
Association and insulin regulated translocation of hormone-sensitive lipase with PTRF.
In vitro stereoselective hydrolysis of diacylglycerols by hormone-sensitive lipase.
A reference map of the human binary protein interactome.
Hormone-sensitive lipase: sequence, expression, and chromosomal localization to 19 cent-q13.3.
Molecular cloning, genomic organization, and expression of a testicular isoform of hormone-sensitive lipase.
file:human/LIPE/LIPE-deep-research-falcon.md
Falcon deep research synthesis for LIPE

Deep Research

Falcon

(LIPE-deep-research-falcon.md)
Research Report: Human **LIPE** (Hormone‑Sensitive Lipase; HSL) — Functional Annotation and Translational Relevance Falcon Edison Scientific Literature 35 citations 2026-05-11T22:36:46.025656

The research report should be a detailed narrative explaining the function, biological processes, and localization of the gene product. Citations should be given for all claims.

You should prioritize authoritative reviews and primary scientific literature when conducting research. You can supplement
this with annotations you find in gene/protein databases, but these can be outdated or inaccurate.

We are specifically interested in the primary function of the gene - for enzymes, what reaction is catalyzed, and what is the substrate specificity? For transporters, what is the substrate? For structural proteins or adapters, what is the broader structural role? For signaling molecules, what is the role in the pathway.

We are interested in where in or outside the cell the gene product carries out its function.

We are also interested in the signaling or biochemical pathways in which the gene functions. We are less interested in broad pleiotropic effects, except where these elucidate the precise role.

Include evidence where possible. We are interested in both experimental evidence as well as inference from structure, evolution, or bioinformatic analysis. Precise studies should be prioritized over high-throughput, where available.

Research Report: Human LIPE (Hormone‑Sensitive Lipase; HSL) — Functional Annotation and Translational Relevance

0. Target verification (critical identity check)

The UniProt accession Q05469 corresponds to human hormone‑sensitive lipase (HSL) encoded by LIPE. A recent mechanistic study explicitly states that the “HSL in our study refers to the adipocyte isoform of human HSL (UniProt: Q05469‑2)” and analyzes its structure and lipid‑droplet binding determinants, thereby directly confirming the UniProt→gene/protein mapping for the human target in question. (peng2025moleculardeterminantsfor pages 1-2)

1. Key concepts and definitions (current understanding)

1.1 What LIPE/HSL is

Hormone‑sensitive lipase (HSL) is an intracellular, neutral serine hydrolase central to regulated mobilization of neutral lipids stored in cytosolic lipid droplets (LDs). In adipocytes it functions in hormonally controlled lipolysis, while in other tissues (e.g., steroidogenic) it contributes to mobilization of esterified sterols and other neutral esters. (nagaroor2023anoverviewof pages 4-7, yang2023regulationoflipolysis pages 1-2)

1.2 Canonical lipolysis pathway position

In the canonical LD lipolysis cascade, ATGL (PNPLA2) initiates triacylglycerol (TAG) breakdown to diacylglycerol (DAG), HSL (LIPE) then preferentially hydrolyzes DAG→monoacylglycerol (MAG) + free fatty acid, and MAG is further hydrolyzed by MAGL to glycerol and fatty acids. This stepwise model is summarized in recent reviews and reinforced in human adipocyte‑focused mechanistic literature. (harake2024involvementofa pages 10-12, poursharifi2025glycerolipidcyclingin pages 16-18, yang2023regulationoflipolysis pages 1-2)

1.3 Enzymatic activities and substrate scope

HSL has broad substrate specificity, with reported activity against TAG, DAG, MAG, cholesteryl esters, retinyl esters, and other esters; multiple sources emphasize that activity toward DAG is markedly higher than toward TAG, positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase. (nagaroor2023anoverviewof pages 7-10, nagaroor2023anoverviewof pages 4-7, poursharifi2025glycerolipidcyclingin pages 16-18)

1.4 Catalytic machinery (biochemical definition)

Human HSL is a classical serine hydrolase with the catalytic triad Ser424–Asp693–His723 and a conserved GXSXG motif. A 2025 biochemical/structural study validates catalytic Ser424 experimentally: the S424A substitution abolishes enzymatic activity in their assay system. (peng2025moleculardeterminantsfor pages 1-2, nagaroor2023anoverviewof pages 7-10)

2. Molecular function: reactions, specificity, and determinants

2.1 Reaction chemistry and quantitative kinetics

A recent recombinant human HSL study reports hydrolysis of p‑nitrophenyl butyrate with Km = 186.1 μM and kcat = 124.5 s−1, providing modern kinetic evidence for catalytic competence of the expressed human enzyme and a benchmark assay used in mechanistic dissection. (peng2025moleculardeterminantsfor pages 1-2)

2.2 Lipid‑droplet association: localization and structural determinants

Cellular localization concept. In adipocytes, HSL is commonly described as largely cytosolic basally and recruited to the lipid droplet surface upon pro‑lipolytic stimulation, where it gains access to neutral lipid substrates within LDs. (yang2023regulationoflipolysis pages 1-2)

Recent structural advance (mechanism of LD binding). A cryo‑EM structure of human HSL (3.4 Å) combined with hydrogen–deuterium exchange MS and cell/biochemical assays identifies two intrinsic LD‑binding motifs:
- residues 489–538, termed the “H‑motif”
- an N‑terminal 4‑helix bundle
Importantly, this work reports that LD binding mediated by these motifs is independent of PKA‑catalyzed phosphorylation, refining (but not negating) the classic phosphorylation/translocation model by separating “intrinsic binding determinants” from “hormonal/PKA regulation.” (peng2025moleculardeterminantsfor pages 1-2)

Figure‑level evidence. The same paper provides figure evidence for (i) overall HSL architecture/organization and (ii) mapping of LD‑binding elements and assay schematics used to test binding to (artificial) lipid droplets. (peng2025moleculardeterminantsfor media 06b3eac4, peng2025moleculardeterminantsfor media 5041a669)

3. Regulation and pathway integration (recently emphasized mechanisms)

3.1 cAMP/PKA axis and LD access control via perilipin

In adipocytes, catecholamine/β‑adrenergic signaling elevates cAMP and activates PKA, which phosphorylates components of the LD lipolysis machinery (notably PLIN1 and HSL) and thereby promotes stimulated lipolysis. A 2024 review emphasizes that PLIN1 phosphorylation recruits HSL to LDs to permit hydrolysis, while PLIN1 dephosphorylation blocks access and inhibits lipolysis. (harake2024involvementofa pages 10-12)

3.2 Human adipocyte LD interactome (2023) and “human‑forward” regulation

A human adipocyte lipid‑droplet proximity labeling study catalogued PLIN1 interactors and identified LIPE among proteins interacting with PLIN1 on lipid droplets; it also reiterates the canonical model that HSL is phosphorylated by PKA and translocates to LDs to perform hydrolysis, while noting that much mechanistic dogma historically derives from non‑human systems—motivating direct study in human adipocytes. (yang2023regulationoflipolysis pages 1-1, yang2023regulationoflipolysis pages 1-2)

3.3 Alternative physiological control of lipolysis (2024 Nature)

A 2024 Nature study describes oxytocin (OXT) as an endogenous regulator of adipose lipolysis in mice and humans and provides quantitative physiological readouts including ~1.6‑fold increased glycerol release from differentiated mouse adipocytes and a similar effect in human adipose explants. It also distinguishes OXT‑driven lipolysis from the classic PKA route: PKA inhibition blocks isoproterenol‑induced lipolysis but does not affect OXT‑induced lipolysis in their assays, while ERK pathway inhibitors reduce OXT‑induced glycerol release—supporting an ERK‑dependent alternative pathway that converges on lipolysis outputs without necessarily operating through the canonical cAMP/PKA module in the same manner. (li2024controloflipolysis pages 1-5)

4. Physiological roles and tissue context (2023–2024 highlights)

4.1 Systemic energy mobilization from adipose lipid droplets

HSL is repeatedly positioned as a “core effector” of LD‑based lipolysis in adipocytes, generating fatty acids and glycerol for systemic use during energy demand. (yang2023regulationoflipolysis pages 1-2)

4.2 Vitamin A (retinoid) mobilization — key 2024 development

A 2024 EMBO Reports study provides mechanistic physiology linking HSL to systemic retinoid homeostasis: adipocyte HSL is required to maintain circulating retinol and RBP4 during fasting in mice; apo‑RBP4 induces retinol release by adipocytes in an HSL‑dependent manner; and HSL deficiency leads to retinoid accumulation in adipose tissue with a drop in serum retinol and RBP4 and downstream effects in eye and kidney. This supports HSL as a major adipose retinyl ester hydrolase in vivo during fasting. (steinhoff2024adipocytehslis pages 1-2)

5. Disease relevance and real‑world implementations

5.1 Monogenic disease: LIPE‑related familial partial lipodystrophy (FPLD6)

Clinical definition and rarity. A 2024 case report notes that familial partial lipodystrophy (FPLD) is rare (~1 in 1,000,000) and underscores genetic testing importance in young patients with severe metabolic syndromes. (zhou2024casereportfirst pages 1-2)

2024 patient report (new variants; concrete phenotype). Zhou et al. (publication month July 2024, URL https://doi.org/10.3389/fgene.2024.1417613) report the first Chinese FPLD6 patient with compound heterozygous LIPE frameshift variants (p.Glu833LysfsTer22 and p.Ser902ThrfsTer27). Reported clinical features include pronounced partial lipodystrophy, hypertriglyceridemia, diabetes mellitus, hepatomegaly/hepatic steatosis, and additional findings (e.g., retinal changes, peripheral neuropathy, renal tubular injury markers). (zhou2024casereportfirst pages 3-5, zhou2024casereportfirst pages 1-2)

Mechanistic interpretation used clinically. The same report explains the mechanistic plausibility: LIPE encodes HSL, which hydrolyzes intracellular triglycerides to free fatty acids in adipose tissue and participates in neutral‑ester hydrolysis in other tissues—linking loss of HSL function to impaired lipid mobilization, fat redistribution, and metabolic complications. (zhou2024casereportfirst pages 1-2)

Synthesis across human reports (review perspective). A 2024 review focused on LD‑pathway genes summarizes that a LIPE null variant was identified in three human subjects with a consistent adult‑onset phenotype including lower‑extremity lipoatrophy, facial/nuchal fat accumulation, insulin resistance/diabetes, hypertriglyceridemia, hepatic steatosis, hypertension, and myopathy; patient‑derived adipose stem cells lacking HSL show impaired adipogenic differentiation, decreased insulin sensitivity, impaired lipolysis, and altered mitochondrial metabolism in the cited work. (harake2024involvementofa pages 12-13, harake2024involvementofa pages 10-12)

5.2 Systems biology/knowledgebase associations (Open Targets)

Open Targets lists LIPE associations with LIPE‑related familial partial lipodystrophy and familial partial lipodystrophy (Dunnigan type) among other links, and it also reports an association with azoospermia (evidence items include curated and literature sources). This is best viewed as a hypothesis‑generating aggregation of evidence rather than mechanistic proof on its own. (OpenTargets Search: -LIPE)

6. Pharmacology and experimental considerations (applications and pitfalls)

6.1 HSL as an off‑target in lipid‑hydrolase inhibitor development (2023)

A 2023 Nature Communications study (publication month December 2023, URL https://doi.org/10.1038/s41467-023-43606-3) describing the peripherally restricted MAGL inhibitor LEI‑515 reports that chemical proteomics identified HSL (LIPE) as the main off‑target in multiple tissues and that this was confirmed by gel‑based activity‑based protein profiling using recombinant human/mouse HSL in HEK293T membranes. The paper therefore cautions that HSL inhibition should be considered when interpreting biological effects attributed solely to MAGL blockade. (jiang2023amonoacylglycerollipase pages 5-6, jiang2023amonoacylglycerollipase pages 10-11)

Quantitatively, the paper reports MAGL IC50 = 25 nM (mouse brain proteome) and large selectivity margins over several other hydrolases/receptors (e.g., >500‑fold over DAGL‑α and ABHD6/12), but the excerpted text does not provide a numeric IC50 for HSL specifically—only identifying it as the main off‑target by ABPP/proteomics. (jiang2023amonoacylglycerollipase pages 5-6)

6.2 Interpreting phenotypes in vivo: “confounding vs limited contribution”

The same 2023 study notes that although LEI‑515 has HSL off‑target activity, phenotypes in their tested disease models were recapitulated by other MAGL inhibitors and MAGL knockout, leading the authors to conclude that HSL plays a limited role, if any, in those specific pathophysiological contexts; nonetheless, they explicitly state that LEI‑515’s HSL inhibitory activity should be considered, particularly in peripheral tissues where HSL can contribute to MAG pools. (jiang2023amonoacylglycerollipase pages 9-10)

7. Recent developments and “expert” synthesis (2023–2025)

7.1 2025 cryo‑EM structure refines mechanistic thinking

The 2025 Nature Communications structural paper provides a major mechanistic advance by defining physical determinants of LD association (H‑motif; N‑terminal 4‑helix bundle) and reporting phosphorylation‑independent LD binding in their system—shifting the field from a purely phosphorylation‑centric view to a combined model in which intrinsic binding motifs and phosphorylation‑dependent signaling cooperate to regulate LD engagement and lipolysis. (peng2025moleculardeterminantsfor pages 1-2)

7.2 2023–2024 shift toward human‑native systems

Human adipocyte LD proteomics (2023) and high‑quality metabolic disease reviews (2023–2024) increasingly emphasize direct human LD biology and human genetics (FPLD6) as anchors for causal inference, complementing mouse‑dominant mechanistic frameworks. (yang2023regulationoflipolysis pages 1-2, zadoorian2023lipiddropletbiogenesis pages 6-7, harake2024involvementofa pages 12-13)

8. Summary table (high‑level functional annotation)

The following table consolidates verified identity, biochemical function, regulation, localization, genetic disease links, and pharmacology considerations for LIPE/HSL (Q05469).

Aspect Current understanding Recent 2023-2025 evidence Key citations
Identity LIPE encodes human hormone-sensitive lipase (HSL), a neutral serine hydrolase in the GDXG lipase family that acts in intracellular neutral-lipid mobilization. Recent primary literature explicitly maps human HSL to UniProt Q05469, with the adipocyte isoform designated Q05469-2. A 2025 cryo-EM/biochemistry study explicitly states that the analyzed human HSL is UniProt Q05469-2 and confirms its role in canonical lipolysis as the diacylglycerol (DAG) lipase step. Human adipocyte studies and 2024 reviews consistently treat LIPE/HSL as a core lipid-droplet lipase. (peng2025moleculardeterminantsfor pages 1-2, yang2023regulationoflipolysis pages 1-2)
Enzymatic reaction In the canonical adipocyte lipolysis cascade, ATGL first hydrolyzes TAG to DAG, HSL preferentially hydrolyzes DAG to MAG, and MAG is then hydrolyzed by MAGL to glycerol plus fatty acid. HSL is therefore the principal DAG lipase in regulated lipolysis, although it also hydrolyzes other neutral esters. Recent reviews and primary studies continue to place HSL centrally in DAG hydrolysis during hormonally stimulated lipolysis. The 2025 structural paper reiterates this step and experimentally validates catalytic activity in recombinant human HSL. (peng2025moleculardeterminantsfor pages 1-2, harake2024involvementofa pages 10-12, poursharifi2025glycerolipidcyclingin pages 16-18, yang2023regulationoflipolysis pages 1-2)
Substrates/specificity HSL has broad substrate specificity, acting on DAG, TAG, MAG, cholesteryl esters, and retinyl esters, but it strongly prefers DAG over TAG. This broad specificity explains its roles in adipocyte lipolysis, steroidogenic cholesterol mobilization, and retinoid homeostasis. A 2024 adipocyte study identifies HSL as the major retinyl ester hydrolase in adipose tissue during fasting. A 2023 review summarizes that human HSL hydrolyzes multiple lipid esters with DAG activity markedly exceeding TAG activity. (nagaroor2023anoverviewof pages 7-10, nagaroor2023anoverviewof pages 4-7, steinhoff2024adipocytehslis pages 1-2)
Catalytic residues Human HSL contains the classical serine-hydrolase catalytic triad Ser424-Asp693-His723 and the conserved GXSXG motif. Catalysis depends on the active-site serine, consistent with inhibition by generic serine-reactive inhibitors. The 2025 cryo-EM/biochemistry study reports that S424A abolishes activity, directly validating Ser424 as essential. The 2023 review independently summarizes Ser424, Asp693, and His723 as the catalytic triad in human HSL. (peng2025moleculardeterminantsfor pages 1-2, nagaroor2023anoverviewof pages 7-10)
Structure/domains HSL comprises an N-terminal regulatory/lipid-binding region and a C-terminal catalytic α/β-hydrolase region. Domain architecture includes an N-terminal 4-helix bundle and a regulatory region that contains phosphorylation and lipid-droplet interaction determinants. A 2025 cryo-EM structure of human HSL at 3.4 Å resolved its homodimeric architecture and identified lipid-droplet binding determinants. Figure evidence in that paper maps the domain architecture and key motifs. (peng2025moleculardeterminantsfor pages 1-2, peng2025moleculardeterminantsfor media 06b3eac4, peng2025moleculardeterminantsfor media 9c4ad302)
Lipid droplet localization HSL is largely cytosolic basally and relocates to the lipid-droplet (LD) surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated droplets. LD recruitment is a major regulatory step controlling substrate access. Human adipocyte proximity-labeling identified LIPE among PLIN1-interacting LD proteins in 2023. The 2025 structure/mechanism paper identified two intrinsic LD-binding elements: residues 489-538 (the “H-motif”) and the N-terminal 4-helix bundle; LD binding in that system was phosphorylation-independent. (yang2023regulationoflipolysis pages 1-1, yang2023regulationoflipolysis pages 1-2, peng2025moleculardeterminantsfor pages 1-2, peng2025moleculardeterminantsfor media 06b3eac4)
Regulation/signaling Classical activation occurs through β-adrenergic/Gs/cAMP/PKA signaling, with PKA phosphorylation of HSL and PLIN1 promoting lipolysis and HSL access to LDs; insulin antagonizes this program. PLIN1 phosphorylation is a key gatekeeper for HSL recruitment to droplets. Recent human adipocyte work confirms cAMP-regulated LD lipolysis machinery, while a 2025 study refines the model by showing that intrinsic LD binding can occur independently of PKA phosphorylation. Additional 2024 work shows alternative lipolytic control pathways, such as oxytocin/ERK signaling, can enhance glycerol release without engaging canonical PKA in the same way. (harake2024involvementofa pages 10-12, yang2023regulationoflipolysis pages 1-2, peng2025moleculardeterminantsfor pages 1-2, li2024controloflipolysis pages 1-5)
Physiological roles LIPE/HSL mobilizes fatty acids from adipocyte lipid droplets for systemic energy supply, contributes to cholesteryl ester hydrolysis in steroidogenic tissues, and participates in retinoid mobilization. It also influences adipocyte differentiation/signaling through ligand generation that may affect PPARγ activity. In 2024, adipocyte HSL was shown to be required for maintenance of circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A role. Recent disease-focused reviews also link LIPE deficiency to impaired endogenous PPARγ ligand generation and adipose dysfunction. (steinhoff2024adipocytehslis pages 1-2, zadoorian2023lipiddropletbiogenesis pages 6-7)
Disease genetics Biallelic loss-of-function LIPE variants cause familial partial lipodystrophy type 6 / LIPE-related familial partial lipodystrophy, with abnormal fat distribution and severe metabolic complications. Reported manifestations include diabetes, hypertriglyceridemia, hepatic steatosis, myopathy, and sometimes retinal, renal, or neurologic findings. A 2024 case report described the first Chinese FPLD6 patient with compound heterozygous pathogenic frameshifts (p.Glu833LysfsTer22 and p.Ser902ThrfsTer27) and a phenotype including diabetes, hypertriglyceridemia, fatty liver, retinal changes, neuropathy, and renal tubular injury. Open Targets also lists LIPE associations with LIPE-related familial partial lipodystrophy and azoospermia. (zhou2024casereportfirst pages 3-5, zhou2024casereportfirst pages 1-2, harake2024involvementofa pages 10-12, OpenTargets Search: -LIPE)
Pharmacology/off-target HSL can be inhibited by generic serine-reactive inhibitors, but selective clinical pharmacology for HSL itself remains limited. A practical issue in lipid-hydrolase drug discovery is that HSL may appear as an off-target when compounds are developed against nearby serine hydrolases. In a 2023 Nature Communications MAGL inhibitor study, LEI-515 was profiled as a potent MAGL inhibitor but HSL/LIPE emerged as the main off-target by chemical proteomics and ABPP. The authors caution that HSL inhibition should be considered when interpreting peripheral MAGL biology, even though comparison with MAGL knockout and other MAGL inhibitors suggested limited HSL contribution in their tested disease models. (jiang2023amonoacylglycerollipase pages 5-6, jiang2023amonoacylglycerollipase pages 10-11, jiang2023amonoacylglycerollipase pages 9-10, jiang2023amonoacylglycerollipase pages 6-6)
Key quantitative data Quantitative biochemical and physiological values support LIPE function. Recombinant human HSL showed p-nitrophenyl butyrate hydrolysis with Km = 186.1 µM and kcat = 124.5 s^-1, and DAG hydrolysis has been reported as substantially greater than TAG hydrolysis. LEI-515 inhibited MAGL in mouse brain proteome with IC50 = 25 nM and showed reported selectivity of >500-fold over DAGL-α and ABHD6/12 and >100-fold over a broader enzyme/receptor panel, although no numeric HSL IC50 was given in the cited excerpt. In physiology, oxytocin increased glycerol release from adipocytes by ~1.6-fold, and HSL-null mouse models cited in recent reviews showed ~2.5-fold higher LD-TAG and ~30% lower basal plasma NEFAs. (peng2025moleculardeterminantsfor pages 1-2, nagaroor2023anoverviewof pages 7-10, li2024controloflipolysis pages 1-5, jiang2023amonoacylglycerollipase pages 5-6, harake2024involvementofa pages 12-13)

Table: This table summarizes verified identity, biochemistry, regulation, localization, disease relevance, and pharmacology for human LIPE/HSL (UniProt Q05469). It emphasizes recent 2023-2025 evidence and includes quantitative values where available.

9. Key references (URLs and publication dates)

  • Yang et al. May 2023. Regulation of lipolysis by 14-3-3 proteins on human adipocyte lipid droplets. PNAS Nexus. https://doi.org/10.1093/pnasnexus/pgad420 (yang2023regulationoflipolysis pages 1-2)
  • Zadoorian et al. May 2023. Lipid droplet biogenesis and functions in health and disease. Nat Rev Endocrinol. https://doi.org/10.1038/s41574-023-00845-0 (zadoorian2023lipiddropletbiogenesis pages 6-7)
  • Jiang et al. Dec 2023. A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence. Nat Commun. https://doi.org/10.1038/s41467-023-43606-3 (jiang2023amonoacylglycerollipase pages 5-6)
  • Steinhoff et al. May 2024. Adipocyte HSL is required for maintaining circulating vitamin A and RBP4 levels during fasting. EMBO Reports. https://doi.org/10.1038/s44319-024-00158-x (steinhoff2024adipocytehslis pages 1-2)
  • Zhou et al. Jul 2024. Case report: First Chinese patient with family partial lipodystrophy type 6 due to novel compound heterozygous mutations in the LIPE gene. Front Genet. https://doi.org/10.3389/fgene.2024.1417613 (zhou2024casereportfirst pages 1-2)
  • Li et al. Sep 2024. Control of lipolysis by a population of oxytocinergic sympathetic neurons. Nature. https://doi.org/10.1101/2022.09.27.509745 (li2024controloflipolysis pages 1-5)
  • Al Harake et al. Sep 2024. Involvement of a battery of investigated genes in lipid droplet pathophysiology and associated comorbidities. Adipocyte. https://doi.org/10.1080/21623945.2024.2403380 (harake2024involvementofa pages 12-13)
  • Peng et al. Apr 2025. Molecular determinants for the association of human hormone-sensitive lipase with lipid droplets. Nat Commun. https://doi.org/10.1038/s41467-025-58887-z (peng2025moleculardeterminantsfor pages 1-2)

References

  1. (peng2025moleculardeterminantsfor pages 1-2): Han Peng, Qikui Xu, Ting Zhang, Jiakai Zhu, Jinheng Pan, Xiaoyu Guan, Shan Feng, Jianping Wu, and Qiuyu Hu. Molecular determinants for the association of human hormone-sensitive lipase with lipid droplets. Nature Communications, Apr 2025. URL: https://doi.org/10.1038/s41467-025-58887-z, doi:10.1038/s41467-025-58887-z. This article has 10 citations and is from a highest quality peer-reviewed journal.

  2. (nagaroor2023anoverviewof pages 4-7): Vijayalakshmi Nagaroor and Sathyanarayana N. Gummadi. An overview of mammalian and microbial hormone-sensitive lipases (lipolytic family iv): biochemical properties and industrial applications. Biotechnology and Genetic Engineering Reviews, 39:281-310, Sep 2023. URL: https://doi.org/10.1080/02648725.2022.2127071, doi:10.1080/02648725.2022.2127071. This article has 9 citations and is from a peer-reviewed journal.

  3. (yang2023regulationoflipolysis pages 1-2): Qin Yang, Zinger Yang Loureiro, Anand Desai, Tiffany DeSouza, Kaida Li, Hui Wang, Sarah M Nicoloro, Javier Solivan-Rivera, and Silvia Corvera. Regulation of lipolysis by 14-3-3 proteins on human adipocyte lipid droplets. PNAS Nexus, May 2023. URL: https://doi.org/10.1093/pnasnexus/pgad420, doi:10.1093/pnasnexus/pgad420. This article has 13 citations and is from a peer-reviewed journal.

  4. (harake2024involvementofa pages 10-12): Sami N. Al Harake, Yasamin Abedin, Fatema Hatoum, Nour Zahraa Nassar, Ali Ali, Aline Nassar, Amjad Kanaan, Samer Bazzi, Sami Azar, Frederic Harb, and Hilda E. Ghadieh. Involvement of a battery of investigated genes in lipid droplet pathophysiology and associated comorbidities. Adipocyte, Sep 2024. URL: https://doi.org/10.1080/21623945.2024.2403380, doi:10.1080/21623945.2024.2403380. This article has 2 citations.

  5. (poursharifi2025glycerolipidcyclingin pages 16-18): Pegah Poursharifi, S. R. Murthy Madiraju, Abel Oppong, Shingo Kajimura, Christopher J. Nolan, Denis P. Blondin, and Marc Prentki. Glycerolipid cycling in thermogenesis, energy homeostasis, signaling, and diseases. Physiological Reviews, 105:2449-2499, Oct 2025. URL: https://doi.org/10.1152/physrev.00024.2024, doi:10.1152/physrev.00024.2024. This article has 13 citations and is from a highest quality peer-reviewed journal.

  6. (nagaroor2023anoverviewof pages 7-10): Vijayalakshmi Nagaroor and Sathyanarayana N. Gummadi. An overview of mammalian and microbial hormone-sensitive lipases (lipolytic family iv): biochemical properties and industrial applications. Biotechnology and Genetic Engineering Reviews, 39:281-310, Sep 2023. URL: https://doi.org/10.1080/02648725.2022.2127071, doi:10.1080/02648725.2022.2127071. This article has 9 citations and is from a peer-reviewed journal.

  7. (peng2025moleculardeterminantsfor media 06b3eac4): Han Peng, Qikui Xu, Ting Zhang, Jiakai Zhu, Jinheng Pan, Xiaoyu Guan, Shan Feng, Jianping Wu, and Qiuyu Hu. Molecular determinants for the association of human hormone-sensitive lipase with lipid droplets. Nature Communications, Apr 2025. URL: https://doi.org/10.1038/s41467-025-58887-z, doi:10.1038/s41467-025-58887-z. This article has 10 citations and is from a highest quality peer-reviewed journal.

  8. (peng2025moleculardeterminantsfor media 5041a669): Han Peng, Qikui Xu, Ting Zhang, Jiakai Zhu, Jinheng Pan, Xiaoyu Guan, Shan Feng, Jianping Wu, and Qiuyu Hu. Molecular determinants for the association of human hormone-sensitive lipase with lipid droplets. Nature Communications, Apr 2025. URL: https://doi.org/10.1038/s41467-025-58887-z, doi:10.1038/s41467-025-58887-z. This article has 10 citations and is from a highest quality peer-reviewed journal.

  9. (yang2023regulationoflipolysis pages 1-1): Qin Yang, Zinger Yang Loureiro, Anand Desai, Tiffany DeSouza, Kaida Li, Hui Wang, Sarah M Nicoloro, Javier Solivan-Rivera, and Silvia Corvera. Regulation of lipolysis by 14-3-3 proteins on human adipocyte lipid droplets. PNAS Nexus, May 2023. URL: https://doi.org/10.1093/pnasnexus/pgad420, doi:10.1093/pnasnexus/pgad420. This article has 13 citations and is from a peer-reviewed journal.

  10. (li2024controloflipolysis pages 1-5): Erwei Li, Luhong Wang, Daqing Wang, Jingyi Chi, Gordon I. Smith, Samuel Klein, Paul Cohen, and Evan D. Rosen. Control of lipolysis by a population of oxytocinergic sympathetic neurons. Nature, 625:175-180, Sep 2024. URL: https://doi.org/10.1101/2022.09.27.509745, doi:10.1101/2022.09.27.509745. This article has 45 citations and is from a highest quality peer-reviewed journal.

  11. (steinhoff2024adipocytehslis pages 1-2): Julia S. Steinhoff, Carina Wagner, Henriette E. Dähnhardt, Kristina Košić, Yueming Meng, U. Taschler, Laura Pajed, Na Yang, Sascha Wulff, Marie F. Kiefer, Konstantin M. Petricek, Roberto E Flores, Chen Li, Sarah Dittrich, Manuela Sommerfeld, Hervé Guillou, Andrea Henze, Jens Raila, Sylvia J Wowro, Gabriele Schoiswohl, A. Lass, and M. Schupp. Adipocyte hsl is required for maintaining circulating vitamin a and rbp4 levels during fasting. EMBO Reports, 25:2878-2895, May 2024. URL: https://doi.org/10.1038/s44319-024-00158-x, doi:10.1038/s44319-024-00158-x. This article has 16 citations and is from a highest quality peer-reviewed journal.

  12. (zhou2024casereportfirst pages 1-2): Yimeng Zhou, Lin Zhang, Yang Ding, and Yongzhen Zhai. Case report: first chinese patient with family partial lipodystrophy type 6 due to novel compound heterozygous mutations in the lipe gene. Frontiers in Genetics, Jul 2024. URL: https://doi.org/10.3389/fgene.2024.1417613, doi:10.3389/fgene.2024.1417613. This article has 5 citations and is from a peer-reviewed journal.

  13. (zhou2024casereportfirst pages 3-5): Yimeng Zhou, Lin Zhang, Yang Ding, and Yongzhen Zhai. Case report: first chinese patient with family partial lipodystrophy type 6 due to novel compound heterozygous mutations in the lipe gene. Frontiers in Genetics, Jul 2024. URL: https://doi.org/10.3389/fgene.2024.1417613, doi:10.3389/fgene.2024.1417613. This article has 5 citations and is from a peer-reviewed journal.

  14. (harake2024involvementofa pages 12-13): Sami N. Al Harake, Yasamin Abedin, Fatema Hatoum, Nour Zahraa Nassar, Ali Ali, Aline Nassar, Amjad Kanaan, Samer Bazzi, Sami Azar, Frederic Harb, and Hilda E. Ghadieh. Involvement of a battery of investigated genes in lipid droplet pathophysiology and associated comorbidities. Adipocyte, Sep 2024. URL: https://doi.org/10.1080/21623945.2024.2403380, doi:10.1080/21623945.2024.2403380. This article has 2 citations.

  15. (OpenTargets Search: -LIPE): Open Targets Query (-LIPE, 29 results). Buniello, A. et al. (2025). Open Targets Platform: facilitating therapeutic hypotheses building in drug discovery. Nucleic Acids Research.

  16. (jiang2023amonoacylglycerollipase pages 5-6): Ming Jiang, Mirjam C. W. Huizenga, Jonah L. Wirt, Janos Paloczi, Avand Amedi, Richard J. B. H. N. van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F. Driever, Bogdan I. Florea, Uwe Grether, Antonius P. A. Janssen, Thomas Hankemeier, Laura H. Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F. Stevens, Daan van der Vliet, Tom van der Wel, Matthias B. Wittwer, Constant A. A. van Boeckel, Pal Pacher, Andrea G. Hohmann, and Mario van der Stelt. A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence. Nature Communications, Dec 2023. URL: https://doi.org/10.1038/s41467-023-43606-3, doi:10.1038/s41467-023-43606-3. This article has 62 citations and is from a highest quality peer-reviewed journal.

  17. (jiang2023amonoacylglycerollipase pages 10-11): Ming Jiang, Mirjam C. W. Huizenga, Jonah L. Wirt, Janos Paloczi, Avand Amedi, Richard J. B. H. N. van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F. Driever, Bogdan I. Florea, Uwe Grether, Antonius P. A. Janssen, Thomas Hankemeier, Laura H. Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F. Stevens, Daan van der Vliet, Tom van der Wel, Matthias B. Wittwer, Constant A. A. van Boeckel, Pal Pacher, Andrea G. Hohmann, and Mario van der Stelt. A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence. Nature Communications, Dec 2023. URL: https://doi.org/10.1038/s41467-023-43606-3, doi:10.1038/s41467-023-43606-3. This article has 62 citations and is from a highest quality peer-reviewed journal.

  18. (jiang2023amonoacylglycerollipase pages 9-10): Ming Jiang, Mirjam C. W. Huizenga, Jonah L. Wirt, Janos Paloczi, Avand Amedi, Richard J. B. H. N. van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F. Driever, Bogdan I. Florea, Uwe Grether, Antonius P. A. Janssen, Thomas Hankemeier, Laura H. Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F. Stevens, Daan van der Vliet, Tom van der Wel, Matthias B. Wittwer, Constant A. A. van Boeckel, Pal Pacher, Andrea G. Hohmann, and Mario van der Stelt. A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence. Nature Communications, Dec 2023. URL: https://doi.org/10.1038/s41467-023-43606-3, doi:10.1038/s41467-023-43606-3. This article has 62 citations and is from a highest quality peer-reviewed journal.

  19. (zadoorian2023lipiddropletbiogenesis pages 6-7): Armella Zadoorian, Ximing Du, and Hongyuan Yang. Lipid droplet biogenesis and functions in health and disease. Nature Reviews. Endocrinology, 19:1-17, May 2023. URL: https://doi.org/10.1038/s41574-023-00845-0, doi:10.1038/s41574-023-00845-0. This article has 626 citations.

  20. (peng2025moleculardeterminantsfor media 9c4ad302): Han Peng, Qikui Xu, Ting Zhang, Jiakai Zhu, Jinheng Pan, Xiaoyu Guan, Shan Feng, Jianping Wu, and Qiuyu Hu. Molecular determinants for the association of human hormone-sensitive lipase with lipid droplets. Nature Communications, Apr 2025. URL: https://doi.org/10.1038/s41467-025-58887-z, doi:10.1038/s41467-025-58887-z. This article has 10 citations and is from a highest quality peer-reviewed journal.

  21. (jiang2023amonoacylglycerollipase pages 6-6): Ming Jiang, Mirjam C. W. Huizenga, Jonah L. Wirt, Janos Paloczi, Avand Amedi, Richard J. B. H. N. van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F. Driever, Bogdan I. Florea, Uwe Grether, Antonius P. A. Janssen, Thomas Hankemeier, Laura H. Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F. Stevens, Daan van der Vliet, Tom van der Wel, Matthias B. Wittwer, Constant A. A. van Boeckel, Pal Pacher, Andrea G. Hohmann, and Mario van der Stelt. A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence. Nature Communications, Dec 2023. URL: https://doi.org/10.1038/s41467-023-43606-3, doi:10.1038/s41467-023-43606-3. This article has 62 citations and is from a highest quality peer-reviewed journal.

Citations

  1. peng2025moleculardeterminantsfor pages 1-2
  2. yang2023regulationoflipolysis pages 1-2
  3. harake2024involvementofa pages 10-12
  4. li2024controloflipolysis pages 1-5
  5. steinhoff2024adipocytehslis pages 1-2
  6. zhou2024casereportfirst pages 1-2
  7. jiang2023amonoacylglycerollipase pages 5-6
  8. jiang2023amonoacylglycerollipase pages 9-10
  9. zadoorian2023lipiddropletbiogenesis pages 6-7
  10. harake2024involvementofa pages 12-13
  11. nagaroor2023anoverviewof pages 4-7
  12. poursharifi2025glycerolipidcyclingin pages 16-18
  13. nagaroor2023anoverviewof pages 7-10
  14. yang2023regulationoflipolysis pages 1-1
  15. zhou2024casereportfirst pages 3-5
  16. jiang2023amonoacylglycerollipase pages 10-11
  17. jiang2023amonoacylglycerollipase pages 6-6
  18. https://doi.org/10.3389/fgene.2024.1417613
  19. https://doi.org/10.1038/s41467-023-43606-3
  20. https://doi.org/10.1093/pnasnexus/pgad420
  21. https://doi.org/10.1038/s41574-023-00845-0
  22. https://doi.org/10.1038/s44319-024-00158-x
  23. https://doi.org/10.1101/2022.09.27.509745
  24. https://doi.org/10.1080/21623945.2024.2403380
  25. https://doi.org/10.1038/s41467-025-58887-z
  26. https://doi.org/10.1038/s41467-025-58887-z,
  27. https://doi.org/10.1080/02648725.2022.2127071,
  28. https://doi.org/10.1093/pnasnexus/pgad420,
  29. https://doi.org/10.1080/21623945.2024.2403380,
  30. https://doi.org/10.1152/physrev.00024.2024,
  31. https://doi.org/10.1101/2022.09.27.509745,
  32. https://doi.org/10.1038/s44319-024-00158-x,
  33. https://doi.org/10.3389/fgene.2024.1417613,
  34. https://doi.org/10.1038/s41467-023-43606-3,
  35. https://doi.org/10.1038/s41574-023-00845-0,

📄 View Raw YAML

id: Q05469
gene_symbol: LIPE
product_type: PROTEIN
status: COMPLETE
taxon:
  id: NCBITaxon:9606
  label: Homo sapiens
description: 'LIPE encodes hormone-sensitive lipase (HSL), an intracellular neutral-lipid serine hydrolase
  that is recruited from the cytosol to lipid droplets during stimulated lipolysis. Its best-supported
  core catalytic role is hydrolysis of diacylglycerol to monoacylglycerol and fatty acid in the adipocyte
  lipolysis cascade; it also hydrolyzes other neutral esters, including triacylglycerols, cholesteryl
  esters, monoacylglycerols, and retinyl esters in tissue-specific contexts.'
existing_annotations:
  - term:
      id: GO:0004771
      label: sterol ester esterase activity
    evidence_type: IBA
    original_reference_id: GO_REF:0000033
    review:
      summary: Sterol ester esterase activity is supported as a secondary neutral-ester substrate
        activity rather than the central adipocyte DAG-lipase role.
      action: KEEP_AS_NON_CORE
      reason: sterol ester esterase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
        - reference_id: PMID:15716583
          supporting_text: Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis
            of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for
            adrenal steroidogenesis.
  - term:
      id: GO:0004806
      label: triacylglycerol lipase activity
    evidence_type: IBA
    original_reference_id: GO_REF:0000033
    review:
      summary: Triacylglycerol lipase activity is biochemically supported, but HSL is positioned
        primarily as the DAG lipase downstream of ATGL in stimulated lipolysis.
      action: KEEP_AS_NON_CORE
      reason: triacylglycerol lipase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
  - term:
      id: GO:0005829
      label: cytosol
    evidence_type: IBA
    original_reference_id: GO_REF:0000033
    review:
      summary: The cytosol annotation is consistent with basal HSL localization before stimulated
        lipid-droplet recruitment.
      action: ACCEPT
      reason: cytosol is supported as part of LIPE/HSL core lipid-droplet lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0019433
      label: triglyceride catabolic process
    evidence_type: IBA
    original_reference_id: GO_REF:0000033
    review:
      summary: HSL acts within the canonical triglyceride catabolic cascade by hydrolyzing DAG
        produced from TAG.
      action: ACCEPT
      reason: triglyceride catabolic process is supported as part of LIPE/HSL core lipid-droplet
        lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
  - term:
      id: GO:0042572
      label: retinol metabolic process
    evidence_type: IEA
    original_reference_id: GO_REF:0000120
    review:
      summary: Retinol metabolism is supported by recent physiology but is a tissue/context-specific
        secondary role rather than the primary neutral-lipid lipolysis function.
      action: KEEP_AS_NON_CORE
      reason: retinol metabolic process is supported, but it is secondary to the core DAG-lipase
        role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In 2024, adipocyte HSL was shown to be required for maintenance of
            circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A
            role.
  - term:
      id: GO:0004771
      label: sterol ester esterase activity
    evidence_type: IEA
    original_reference_id: GO_REF:0000117
    review:
      summary: Sterol ester esterase activity is supported as a secondary neutral-ester substrate
        activity rather than the central adipocyte DAG-lipase role.
      action: KEEP_AS_NON_CORE
      reason: sterol ester esterase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
        - reference_id: PMID:15716583
          supporting_text: Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis
            of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for
            adrenal steroidogenesis.
  - term:
      id: GO:0004806
      label: triacylglycerol lipase activity
    evidence_type: IEA
    original_reference_id: GO_REF:0000120
    review:
      summary: Triacylglycerol lipase activity is biochemically supported, but HSL is positioned
        primarily as the DAG lipase downstream of ATGL in stimulated lipolysis.
      action: KEEP_AS_NON_CORE
      reason: triacylglycerol lipase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
  - term:
      id: GO:0005811
      label: lipid droplet
    evidence_type: IEA
    original_reference_id: GO_REF:0000044
    review:
      summary: The lipid droplet annotation captures the regulated site where HSL gains access to
        stored neutral lipid substrates.
      action: ACCEPT
      reason: lipid droplet is supported as part of LIPE/HSL core lipid-droplet lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0005829
      label: cytosol
    evidence_type: IEA
    original_reference_id: GO_REF:0000044
    review:
      summary: The cytosol annotation is consistent with basal HSL localization before stimulated
        lipid-droplet recruitment.
      action: ACCEPT
      reason: cytosol is supported as part of LIPE/HSL core lipid-droplet lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0005886
      label: plasma membrane
    evidence_type: IEA
    original_reference_id: GO_REF:0000044
    review:
      summary: Plasma membrane association has experimental support through PTRF/caveola studies,
        but it is not the main functional location of HSL.
      action: KEEP_AS_NON_CORE
      reason: plasma membrane is supported, but it is secondary to the core DAG-lipase role.
      supported_by:
        - reference_id: PMID:17026959
          supporting_text: In the plasma membrane PTRF was specifically bound to a
            triacylglycerol-metabolizing subclass of caveolae containing hormone-sensitive lipase
            (HSL).
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0005901
      label: caveola
    evidence_type: IEA
    original_reference_id: GO_REF:0000044
    review:
      summary: Caveola association is supported in adipocytes through PTRF, but it is secondary to
        cytosol-to-lipid-droplet recruitment during lipolysis.
      action: KEEP_AS_NON_CORE
      reason: caveola is supported, but it is secondary to the core DAG-lipase role.
      supported_by:
        - reference_id: PMID:17026959
          supporting_text: In the plasma membrane PTRF was specifically bound to a
            triacylglycerol-metabolizing subclass of caveolae containing hormone-sensitive lipase
            (HSL).
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0006629
      label: lipid metabolic process
    evidence_type: IEA
    original_reference_id: GO_REF:0000043
    review:
      summary: The generic lipid metabolic process annotation is directionally correct but too broad
        for HSL. Lipid catabolic process, and more specifically diacylglycerol catabolic process,
        better capture the reviewed function.
      action: MODIFY
      reason: lipid metabolic process is less informative than the reviewed LIPE/HSL lipolysis term.
      proposed_replacement_terms:
        - id: GO:0016042
          label: lipid catabolic process
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0008202
      label: steroid metabolic process
    evidence_type: IEA
    original_reference_id: GO_REF:0000043
    review:
      summary: Steroid metabolic process is plausible through cholesteryl ester hydrolysis in
        steroidogenic tissues but is not the central LIPE function.
      action: KEEP_AS_NON_CORE
      reason: steroid metabolic process is supported, but it is secondary to the core DAG-lipase
        role.
      supported_by:
        - reference_id: PMID:15716583
          supporting_text: Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis
            of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for
            adrenal steroidogenesis.
  - term:
      id: GO:0008203
      label: cholesterol metabolic process
    evidence_type: IEA
    original_reference_id: GO_REF:0000120
    review:
      summary: Cholesterol metabolism is supported through cholesteryl ester hydrolysis, but this is
        a secondary substrate context.
      action: KEEP_AS_NON_CORE
      reason: cholesterol metabolic process is supported, but it is secondary to the core DAG-lipase
        role.
      supported_by:
        - reference_id: PMID:15716583
          supporting_text: The relatively higher turnover of HSL on CO observed in vitro adds
            further molecular insight on the physiological importance of HSL in cholesteryl ester
            catabolism in vivo.
  - term:
      id: GO:0016042
      label: lipid catabolic process
    evidence_type: IEA
    original_reference_id: GO_REF:0000120
    review:
      summary: Lipid catabolic process is supported because LIPE/HSL hydrolyzes neutral lipid esters
        during lipolysis.
      action: ACCEPT
      reason: lipid catabolic process is supported as part of LIPE/HSL core lipid-droplet lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0016298
      label: lipase activity
    evidence_type: IEA
    original_reference_id: GO_REF:0000002
    review:
      summary: Generic lipase activity should be refined to diacylglycerol lipase activity because
        DAG hydrolysis is the best-supported core catalytic step.
      action: MODIFY
      reason: lipase activity is less informative than the reviewed LIPE/HSL lipolysis term.
      proposed_replacement_terms:
        - id: GO:0120516
          label: diacylglycerol lipase activity
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0016787
      label: hydrolase activity
    evidence_type: IEA
    original_reference_id: GO_REF:0000120
    review:
      summary: Generic hydrolase activity obscures the specific serine-lipase reaction supported for
        LIPE/HSL.
      action: MODIFY
      reason: hydrolase activity is less informative than the reviewed LIPE/HSL lipolysis term.
      proposed_replacement_terms:
        - id: GO:0120516
          label: diacylglycerol lipase activity
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0047372
      label: monoacylglycerol lipase activity
    evidence_type: IEA
    original_reference_id: GO_REF:0000120
    review:
      summary: Monoacylglycerol lipase activity is consistent with broad HSL substrate specificity,
        but the dominant physiological lipolysis role is DAG hydrolysis.
      action: KEEP_AS_NON_CORE
      reason: monoacylglycerol lipase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0047376
      label: all-trans-retinyl-palmitate hydrolase, all-trans-retinol forming activity
    evidence_type: IEA
    original_reference_id: GO_REF:0000116
    review:
      summary: Retinyl-palmitate hydrolase activity is supported as part of retinoid mobilization
        but should be treated as a secondary substrate-specific function.
      action: KEEP_AS_NON_CORE
      reason: all-trans-retinyl-palmitate hydrolase, all-trans-retinol forming activity is
        supported, but it is secondary to the core DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In 2024, adipocyte HSL was shown to be required for maintenance of
            circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A
            role.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0050253
      label: retinyl-palmitate esterase activity
    evidence_type: IEA
    original_reference_id: GO_REF:0000117
    review:
      summary: Retinyl-palmitate esterase activity is supported as part of retinoid mobilization but
        is secondary to the primary DAG lipase role.
      action: KEEP_AS_NON_CORE
      reason: retinyl-palmitate esterase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In 2024, adipocyte HSL was shown to be required for maintenance of
            circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A
            role.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0120516
      label: diacylglycerol lipase activity
    evidence_type: IEA
    original_reference_id: GO_REF:0000120
    review:
      summary: Diacylglycerol lipase activity is the best-supported core molecular function of HSL.
      action: ACCEPT
      reason: diacylglycerol lipase activity is supported as part of LIPE/HSL core lipid-droplet
        lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0005515
      label: protein binding
    evidence_type: IPI
    original_reference_id: PMID:32296183
    review:
      summary: Protein binding is too generic for curation of LIPE; the reviewed biology is better
        represented by regulated localization to PLIN1-coated lipid droplets and specific lipid
        hydrolase activities.
      action: MARK_AS_OVER_ANNOTATED
      reason: protein binding overstates or obscures the specific supported LIPE function.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0005829
      label: cytosol
    evidence_type: IDA
    original_reference_id: GO_REF:0000052
    review:
      summary: The cytosol annotation is consistent with basal HSL localization before stimulated
        lipid-droplet recruitment.
      action: ACCEPT
      reason: cytosol is supported as part of LIPE/HSL core lipid-droplet lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0019433
      label: triglyceride catabolic process
    evidence_type: IEA
    original_reference_id: GO_REF:0000041
    review:
      summary: HSL acts within the canonical triglyceride catabolic cascade by hydrolyzing DAG
        produced from TAG.
      action: ACCEPT
      reason: triglyceride catabolic process is supported as part of LIPE/HSL core lipid-droplet
        lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
  - term:
      id: GO:0004771
      label: sterol ester esterase activity
    evidence_type: IDA
    original_reference_id: PMID:15716583
    review:
      summary: Sterol ester esterase activity is supported as a secondary neutral-ester substrate
        activity rather than the central adipocyte DAG-lipase role.
      action: KEEP_AS_NON_CORE
      reason: sterol ester esterase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
        - reference_id: PMID:15716583
          supporting_text: Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis
            of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for
            adrenal steroidogenesis.
  - term:
      id: GO:0004771
      label: sterol ester esterase activity
    evidence_type: IDA
    original_reference_id: PMID:8812477
    review:
      summary: Sterol ester esterase activity is supported as a secondary neutral-ester substrate
        activity rather than the central adipocyte DAG-lipase role.
      action: KEEP_AS_NON_CORE
      reason: sterol ester esterase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
        - reference_id: PMID:15716583
          supporting_text: Hormone-sensitive lipase (HSL) contributes importantly to the hydrolysis
            of cholesteryl ester in steroidogenic tissues, releasing the cholesterol required for
            adrenal steroidogenesis.
  - term:
      id: GO:0004806
      label: triacylglycerol lipase activity
    evidence_type: IDA
    original_reference_id: PMID:15716583
    review:
      summary: Triacylglycerol lipase activity is biochemically supported, but HSL is positioned
        primarily as the DAG lipase downstream of ATGL in stimulated lipolysis.
      action: KEEP_AS_NON_CORE
      reason: triacylglycerol lipase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
  - term:
      id: GO:0004806
      label: triacylglycerol lipase activity
    evidence_type: IDA
    original_reference_id: PMID:15955102
    review:
      summary: Triacylglycerol lipase activity is biochemically supported, but HSL is positioned
        primarily as the DAG lipase downstream of ATGL in stimulated lipolysis.
      action: KEEP_AS_NON_CORE
      reason: triacylglycerol lipase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
  - term:
      id: GO:0016020
      label: membrane
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: Generic membrane association is retained as non-core because HSL can associate with
        caveolae and lipid droplets while remaining primarily a regulated soluble lipase.
      action: KEEP_AS_NON_CORE
      reason: membrane is supported, but it is secondary to the core DAG-lipase role.
      supported_by:
        - reference_id: PMID:17026959
          supporting_text: In the plasma membrane PTRF was specifically bound to a
            triacylglycerol-metabolizing subclass of caveolae containing hormone-sensitive lipase
            (HSL).
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0046340
      label: diacylglycerol catabolic process
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: Diacylglycerol catabolic process is the most precise biological-process annotation
        for HSL in the lipolysis cascade.
      action: ACCEPT
      reason: diacylglycerol catabolic process is supported as part of LIPE/HSL core lipid-droplet
        lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
  - term:
      id: GO:0046485
      label: ether lipid metabolic process
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: Ether lipid metabolic process is not supported by the reviewed LIPE literature; the
        evidence supports neutral acylglycerol, sterol ester, and retinyl ester hydrolysis instead.
      action: MARK_AS_OVER_ANNOTATED
      reason: ether lipid metabolic process overstates or obscures the specific supported LIPE
        function.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0047372
      label: monoacylglycerol lipase activity
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: Monoacylglycerol lipase activity is consistent with broad HSL substrate specificity,
        but the dominant physiological lipolysis role is DAG hydrolysis.
      action: KEEP_AS_NON_CORE
      reason: monoacylglycerol lipase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0050253
      label: retinyl-palmitate esterase activity
    evidence_type: IDA
    original_reference_id: PMID:15955102
    review:
      summary: Retinyl-palmitate esterase activity is supported as part of retinoid mobilization but
        is secondary to the primary DAG lipase role.
      action: KEEP_AS_NON_CORE
      reason: retinyl-palmitate esterase activity is supported, but it is secondary to the core
        DAG-lipase role.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In 2024, adipocyte HSL was shown to be required for maintenance of
            circulating retinol and RBP4 during fasting, establishing a concrete systemic vitamin A
            role.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0120516
      label: diacylglycerol lipase activity
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: Diacylglycerol lipase activity is the best-supported core molecular function of HSL.
      action: ACCEPT
      reason: diacylglycerol lipase activity is supported as part of LIPE/HSL core lipid-droplet
        lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0120516
      label: diacylglycerol lipase activity
    evidence_type: IDA
    original_reference_id: PMID:19800417
    review:
      summary: Diacylglycerol lipase activity is the best-supported core molecular function of HSL.
      action: ACCEPT
      reason: diacylglycerol lipase activity is supported as part of LIPE/HSL core lipid-droplet
        lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0120516
      label: diacylglycerol lipase activity
    evidence_type: IDA
    original_reference_id: PMID:8812477
    review:
      summary: Diacylglycerol lipase activity is the best-supported core molecular function of HSL.
      action: ACCEPT
      reason: diacylglycerol lipase activity is supported as part of LIPE/HSL core lipid-droplet
        lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0005811
      label: lipid droplet
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: The lipid droplet annotation captures the regulated site where HSL gains access to
        stored neutral lipid substrates.
      action: ACCEPT
      reason: lipid droplet is supported as part of LIPE/HSL core lipid-droplet lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0016042
      label: lipid catabolic process
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: Lipid catabolic process is supported because LIPE/HSL hydrolyzes neutral lipid esters
        during lipolysis.
      action: ACCEPT
      reason: lipid catabolic process is supported as part of LIPE/HSL core lipid-droplet lipolysis.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
            triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
            preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
            further hydrolyzed by **MAGL** to glycerol and fatty acids.
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL has **broad substrate specificity**, with reported activity against
            **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple
            sources emphasize that activity toward **DAG is markedly higher than toward TAG**,
            positioning HSL as the dominant DAG lipase in stimulated lipolysis rather than the
            initiating TAG lipase.
  - term:
      id: GO:0005515
      label: protein binding
    evidence_type: IPI
    original_reference_id: PMID:17026959
    review:
      summary: Protein binding is too generic for curation of LIPE; the reviewed biology is better
        represented by regulated localization to PLIN1-coated lipid droplets and specific lipid
        hydrolase activities.
      action: MARK_AS_OVER_ANNOTATED
      reason: protein binding overstates or obscures the specific supported LIPE function.
      supported_by:
        - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
          supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
            surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
            droplets. LD recruitment is a major regulatory step controlling substrate access.
  - term:
      id: GO:0006468
      label: protein phosphorylation
    evidence_type: TAS
    original_reference_id: PMID:3420405
    review:
      summary: This annotation treats LIPE as if it performs protein phosphorylation. The cited
        biology describes HSL as a phosphorylation-regulated lipase, not a kinase.
      action: REMOVE
      reason: LIPE is regulated by phosphorylation but does not catalyze protein phosphorylation.
      supported_by:
        - reference_id: PMID:3420405
          supporting_text: Hormone-sensitive lipase, a key enzyme in fatty acid mobilization,
            overall energy homeostasis, and possibly steroidogenesis, is acutely controlled through
            reversible phosphorylation by catecholamines and insulin.
references:
  - id: GO_REF:0000002
    title: Gene Ontology annotation through association of InterPro records with GO terms
    findings: []
  - id: GO_REF:0000024
    title: Manual transfer of experimentally-verified manual GO annotation data to orthologs by
      curator judgment of sequence similarity
    findings: []
  - id: GO_REF:0000033
    title: Annotation inferences using phylogenetic trees
    findings: []
  - id: GO_REF:0000041
    title: Gene Ontology annotation based on UniPathway vocabulary mapping
    findings: []
  - id: GO_REF:0000043
    title: Gene Ontology annotation based on UniProtKB/Swiss-Prot keyword mapping
    findings: []
  - id: GO_REF:0000044
    title: Gene Ontology annotation based on UniProtKB/Swiss-Prot Subcellular Location vocabulary
      mapping, accompanied by conservative changes to GO terms applied by UniProt
    findings: []
  - id: GO_REF:0000052
    title: Gene Ontology annotation based on curation of immunofluorescence data
    findings: []
  - id: GO_REF:0000116
    title: Automatic Gene Ontology annotation based on Rhea mapping
    findings: []
  - id: GO_REF:0000117
    title: Electronic Gene Ontology annotations created by ARBA machine learning models
    findings: []
  - id: GO_REF:0000120
    title: Combined Automated Annotation using Multiple IEA Methods
    findings: []
  - id: PMID:15716583
    title: Continuous monitoring of cholesterol oleate hydrolysis by hormone-sensitive lipase and
      other cholesterol esterases.
    findings: []
  - id: PMID:15955102
    title: Identification of a novel keratinocyte retinyl ester hydrolase as a transacylase and
      lipase.
    findings: []
  - id: PMID:17026959
    title: Association and insulin regulated translocation of hormone-sensitive lipase with PTRF.
    findings: []
  - id: PMID:19800417
    title: In vitro stereoselective hydrolysis of diacylglycerols by hormone-sensitive lipase.
    findings: []
  - id: PMID:32296183
    title: A reference map of the human binary protein interactome.
    findings: []
  - id: PMID:3420405
    title: 'Hormone-sensitive lipase: sequence, expression, and chromosomal localization to 19 cent-q13.3.'
    findings: []
  - id: PMID:8812477
    title: Molecular cloning, genomic organization, and expression of a testicular isoform of
      hormone-sensitive lipase.
    findings: []
  - id: file:human/LIPE/LIPE-deep-research-falcon.md
    title: Falcon deep research synthesis for LIPE
    findings: []
core_functions:
  - description: Cytosol-to-lipid-droplet diacylglycerol lipase activity during hormonally
      stimulated neutral-lipid mobilization.
    molecular_function:
      id: GO:0120516
      label: diacylglycerol lipase activity
    directly_involved_in:
      - id: GO:0046340
        label: diacylglycerol catabolic process
      - id: GO:0019433
        label: triglyceride catabolic process
      - id: GO:0016042
        label: lipid catabolic process
    locations:
      - id: GO:0005829
        label: cytosol
      - id: GO:0005811
        label: lipid droplet
    supported_by:
      - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
        supporting_text: In the canonical LD lipolysis cascade, **ATGL (PNPLA2)** initiates
          triacylglycerol (TAG) breakdown to diacylglycerol (DAG), **HSL (LIPE)** then
          preferentially hydrolyzes **DAG→monoacylglycerol (MAG) + free fatty acid**, and MAG is
          further hydrolyzed by **MAGL** to glycerol and fatty acids.
      - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
        supporting_text: HSL is largely cytosolic basally and relocates to the lipid-droplet (LD)
          surface during stimulated lipolysis, where it interacts functionally with PLIN1-coated
          droplets. LD recruitment is a major regulatory step controlling substrate access.
      - reference_id: file:human/LIPE/LIPE-deep-research-falcon.md
        supporting_text: HSL has **broad substrate specificity**, with reported activity against
          **TAG, DAG, MAG, cholesteryl esters, retinyl esters**, and other esters; multiple sources
          emphasize that activity toward **DAG is markedly higher than toward TAG**, positioning HSL
          as the dominant DAG lipase in stimulated lipolysis rather than the initiating TAG lipase.
proposed_new_terms: []
suggested_questions: []
suggested_experiments: []