PPP4R1

UniProt ID: Q8TF05
Organism: Homo sapiens
Review Status: COMPLETE
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Gene Description

PPP4R1 encodes PP4 regulatory subunit 1, a HEAT/ARM-repeat scaffolding subunit of the serine/threonine protein phosphatase 4 holoenzyme. PPP4R1 binds the catalytic subunit PPP4C to form a PP4C-PPP4R1 complex that directs phosphatase activity toward selected targets. The best-supported PPP4R1-specific process is dampening canonical NF-kappaB signaling through PP4-dependent regulation of TRAF2/TRAF6 and the IKK/NEMO axis. Broader PP4 roles in DNA damage response are well established for PP4 complexes, but the strongest DDR substrate evidence is not specific to the PPP4R1-containing holoenzyme.

Existing Annotations Review

GO Term Evidence Action Reason
GO:0005737 cytoplasm
IBA
GO_REF:0000033
ACCEPT
Summary: Cytoplasmic localization is consistent with PPP4R1 acting in PP4 signaling complexes, although precise compartment-specific localization is not strongly resolved.
Reason: Falcon research notes sparse direct localization evidence but supports cytoplasm as a reasonable broad location for PPP4R1-containing PP4 signaling complexes.
Supporting Evidence:
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
Direct localization data for human PPP4R1 are comparatively sparse; available evidence indicates PP4 regulatory subunits help determine holoenzyme subcellular localization.
GO:0019888 protein phosphatase regulator activity
IBA
GO_REF:0000033
ACCEPT
Summary: PPP4R1 is a non-catalytic regulatory/scaffolding subunit of PP4 that binds PPP4C and helps define holoenzyme substrate targeting.
Reason: This is the most appropriate molecular-function annotation for PPP4R1: it regulates a protein phosphatase rather than catalyzing dephosphorylation itself.
Supporting Evidence:
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1 is a regulatory/scaffolding subunit of the serine/threonine phosphatase PP4.
PMID:10026142
The PP4R1 cDNA clone engineered with an N-terminal Myc tag was expressed in COS M6 cells and PP4C co-immunoprecipitated with Myc-tagged PP4R1.
GO:0005515 protein binding
IPI
PMID:16085932
A novel, evolutionarily conserved protein phosphatase comple...
MODIFY
Summary: This IPI annotation captures PPP4R1 binding to PPP4C, but generic protein binding is less informative than the known PP4 regulatory subunit activity.
Reason: PPP4R1's PPP4C interaction should be represented as protein phosphatase regulator activity rather than the uninformative protein binding term.
Supporting Evidence:
PMID:16085932
Using a combination of tandem affinity purification tagging and mass spectrometry, we characterized a novel, evolutionarily conserved protein phosphatase 4 (PP4)-containing complex.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
A foundational proteomics analysis of human PP4 complexes reported mutually exclusive PP4C assemblies that include a binary PP4C-PPP4R1 complex.
GO:0005515 protein binding
IPI
PMID:17353931
Large-scale mapping of human protein-protein interactions by...
MODIFY
Summary: This high-throughput interactome annotation reports PPP4C binding, but the biologically meaningful interpretation is PPP4 regulator/scaffold activity.
Reason: Replace generic protein binding with the more informative protein phosphatase regulator activity term supported by the PPP4R1-PPP4C complex literature.
Supporting Evidence:
PMID:17353931
Mapping protein-protein interactions is an invaluable tool for understanding protein function.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1 defines a specific PP4 holoenzyme class rather than being a generic interactor.
GO:0005515 protein binding
IPI
PMID:18614045
A PP4-phosphatase complex dephosphorylates gamma-H2AX genera...
REMOVE
Summary: This interaction entry concerns PP4 complex biology, but the cited gamma-H2AX paper primarily supports a PP4R2/PP4R3-containing complex rather than a PPP4R1-specific DDR role.
Reason: The local publication text supports a PP4C/PP4R2/PP4R3beta gamma-H2AX phosphatase complex rather than a PPP4R1-containing complex, so this PMID should not support a PPP4R1 functional annotation.
Supporting Evidence:
PMID:18614045
Here we describe a three-protein PP4 phosphatase complex in mammalian cells, containing PP4C, PP4R2, and PP4R3beta, that specifically dephosphorylates ATR-mediated gamma-H2AX.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
DDR substrate assignments are most often attributed to PP4 complexes broadly or to PP4R2/PP4R3-containing assemblies rather than being conclusively mapped to the PPP4R1-containing heterodimer.
GO:0005515 protein binding
IPI
PMID:18715871
PP4R4/KIAA1622 forms a novel stable cytosolic complex with p...
MODIFY
Summary: This PP4 regulatory-subunit study distinguishes PP4R4 from PP4R1 complexes; the PPP4R1-PPP4C interaction should still be represented by the regulator activity term rather than protein binding.
Reason: Generic protein binding does not capture the role of PPP4R1 as a PP4 regulatory/scaffolding subunit.
Supporting Evidence:
PMID:18715871
PP4c interacts with regulatory proteins, which specify substrate targeting and intracellular localization.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PP4 holoenzymes are members of the PP2A-like phosphoprotein phosphatase family, in which a catalytic subunit associates with regulatory proteins that shape substrate selection, localization, and signaling outputs.
GO:0005515 protein binding
IPI
PMID:26496610
A human interactome in three quantitative dimensions organiz...
MODIFY
Summary: This quantitative interactome annotation is compatible with PPP4R1 interacting with PPP4C, but protein binding is not the best GO representation of the established function.
Reason: Replace with protein phosphatase regulator activity to capture the regulatory-subunit role.
Supporting Evidence:
PMID:26496610
Using quantitative proteomics, we detect specific interactions, estimate interaction stoichiometries, and measure cellular abundances of interacting proteins.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1 is a repeat-rich scaffold protein with PP2A-A-like HEAT repeats, consistent with a regulatory subunit that presents binding surfaces for catalytic subunit and substrates/adaptors.
GO:0005515 protein binding
IPI
PMID:27880917
Phenotypic and Interaction Profiling of the Human Phosphatas...
MODIFY
Summary: The phosphatase interactome result is consistent with PP4 complex membership, but the actionable GO annotation should be PPP4R1's phosphatase regulator role.
Reason: PPP4R1 is not merely a binding protein; it is the regulatory/scaffolding subunit of a PP4 holoenzyme.
Supporting Evidence:
PMID:27880917
We identified 1,335 high-confidence interactions (1,104 previously unreported), implicating these phosphatases in the regulation of a variety of cellular processes.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1's functional contribution is to form a PPP4C-PPP4R1 holoenzyme that can direct PP4 dephosphorylation activity toward specific signaling modules.
GO:0005515 protein binding
IPI
PMID:33961781
Dual proteome-scale networks reveal cell-specific remodeling...
MODIFY
Summary: This proteome-scale interaction supports PPP4C association but is still too generic as a protein binding annotation.
Reason: The PPP4C interaction should be curated as protein phosphatase regulator activity in the PP4 complex context.
Supporting Evidence:
PMID:33961781
Dual proteome-scale networks reveal cell-specific remodeling of the human interactome.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1 is a regulatory/scaffolding subunit of the serine/threonine phosphatase PP4.
GO:0005515 protein binding
IPI
PMID:40205054
Multimodal cell maps as a foundation for structural and func...
MODIFY
Summary: This recent multimodal cell-map interaction should not leave PPP4R1 with a generic protein binding function when the PP4 regulatory role is known.
Reason: Use protein phosphatase regulator activity to capture the functional consequence of PPP4R1 binding PPP4C.
Supporting Evidence:
PMID:40205054
Multimodal cell maps as a foundation for structural and functional genomics.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1 defines a specific PP4 holoenzyme class rather than being a generic interactor.
GO:0004721 phosphoprotein phosphatase activity
ISS
GO_REF:0000024
MODIFY
Summary: This annotation is acceptable only with the contributes_to qualifier, but the broad phosphoprotein phosphatase term should be replaced with the more specific protein serine/threonine phosphatase activity term.
Reason: PPP4R1 forms a complex with serine/threonine phosphatase PPP4C, so contributes_to protein serine/threonine phosphatase activity is defensible, while enables would be misleading.
Supporting Evidence:
PMID:10026142
These data indicate that one form of PP4 is similar to the core complex of PP2A in that it consists of a catalytic subunit and a PP2AA-like structural subunit.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1 itself is not an enzyme; the catalytic activity resides in PPP4C.
GO:0006468 protein phosphorylation
ISS
GO_REF:0000024
REMOVE
Summary: This is an opposite-reaction misannotation. PPP4R1 is a regulatory subunit of protein phosphatase 4, which removes phosphate groups from phosphoproteins rather than phosphorylating them.
Reason: PPP4R1 is not a kinase, and the supported PP4 biology concerns dephosphorylation or regulation of phosphatase activity, not protein phosphorylation.
Supporting Evidence:
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1 itself is not an enzyme; the catalytic activity resides in PPP4C, which hydrolyzes phosphate esters on phosphoserine/ phosphothreonine residues.
GO:0030289 protein phosphatase 4 complex
ISS
GO_REF:0000024
ACCEPT
Summary: PPP4R1 is a component of the PP4C-PPP4R1 protein phosphatase 4 holoenzyme.
Reason: Multiple sources support PPP4R1 as a stable regulatory subunit in a PP4C-PPP4R1 complex.
Supporting Evidence:
PMID:10026142
The final product contained two major proteins: the PP4 catalytic subunit plus a protein that migrated as a doublet of 120-125 kDa.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
In mammals, PP4 can form a heterodimer with PPP4R1 (PP4C/PP4R1) and other distinct assemblies with other regulatory subunits.
GO:0007165 signal transduction
NAS
PMID:10026142
Purification and identification of a novel subunit of protei...
MODIFY
Summary: The broad signal transduction annotation should be replaced by the specific PPP4R1-supported process: negative regulation of canonical NF-kappaB signal transduction.
Reason: PPP4R1-specific pathway evidence supports inhibition of canonical NF-kappaB signaling through TRAF2/TRAF6 and IKK/NEMO, not generic signal transduction.
Supporting Evidence:
PMID:25134449
Exogenous expression of PP4R1 inhibited NF-kappaB activation by TRAF2, TRAF6, TNF and the Epstein-Barr virus oncoprotein LMP1.
PMID:28445980
Formation of a complex with PP4R1 and PP4c is required to bridge MCPyV tAg to the NEMO adaptor protein, allowing deactivation of the NF-kB pathway.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
The best-supported direct biological function of this holoenzyme is negative regulation of inflammatory NF-kappaB signaling.
GO:0019888 protein phosphatase regulator activity
NAS
PMID:10026142
Purification and identification of a novel subunit of protei...
ACCEPT
Summary: The founding biochemical study supports PPP4R1 as a PP4 regulatory subunit that binds PPP4C.
Reason: This is a direct, specific annotation for PPP4R1's core molecular function.
Supporting Evidence:
PMID:10026142
Amino acid sequence information of several peptides derived from the 105 kDa protein was utilized to isolate a human cDNA clone.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
PPP4R1 encodes a HEAT-repeat scaffold regulatory subunit that forms a PP4C-PPP4R1 holoenzyme.

Core Functions

Regulatory/scaffolding subunit of the PP4C-PPP4R1 serine/threonine phosphatase holoenzyme that contributes to phosphoprotein phosphatase activity and directs PP4-dependent negative regulation of canonical NF-kappaB signaling.

Supporting Evidence:
  • PMID:10026142
    PP4C co-immunoprecipitated with Myc-tagged PP4R1.
  • PMID:25134449
    Exogenous expression of PP4R1 inhibited NF-kappaB activation by TRAF2, TRAF6, TNF and the Epstein-Barr virus oncoprotein LMP1.
  • file:human/PPP4R1/PPP4R1-deep-research-falcon.md
    PPP4R1 encodes a HEAT-repeat scaffold regulatory subunit that forms a PP4C-PPP4R1 holoenzyme.

References

Manual transfer of experimentally-verified manual GO annotation data to orthologs by curator judgment of sequence similarity
Annotation inferences using phylogenetic trees
Purification and identification of a novel subunit of protein serine/threonine phosphatase 4.
Cloning and characterization of a novel subunit of protein serine/threonine phosphatase 4 from mesangial cells.
Histone deacetylase 3 (HDAC3) activity is regulated by interaction with protein serine/threonine phosphatase 4.
A novel, evolutionarily conserved protein phosphatase complex involved in cisplatin sensitivity.
Large-scale mapping of human protein-protein interactions by mass spectrometry.
A PP4-phosphatase complex dephosphorylates gamma-H2AX generated during DNA replication.
PP4R4/KIAA1622 forms a novel stable cytosolic complex with phosphoprotein phosphatase 4.
The PP4R1 subunit of protein phosphatase PP4 targets TRAF2 and TRAF6 to mediate inhibition of NF-kappaB activation.
A human interactome in three quantitative dimensions organized by stoichiometries and abundances.
Phenotypic and Interaction Profiling of the Human Phosphatases Identifies Diverse Mitotic Regulators.
The PP4R1 sub-unit of protein phosphatase PP4 is essential for inhibition of NF-kappaB by merkel polyomavirus small tumour antigen.
Dual proteome-scale networks reveal cell-specific remodeling of the human interactome.
Multimodal cell maps as a foundation for structural and functional genomics.
file:human/PPP4R1/PPP4R1-deep-research-falcon.md
Falcon deep research report for human PPP4R1

Suggested Questions for Experts

Q: Which endogenous human substrates are specifically directed by the PPP4R1-containing PP4 holoenzyme rather than by PP4R2/PP4R3 or PP4R4 complexes?

Q: In which cell types is PPP4R1-dependent negative regulation of canonical NF-kappaB signaling physiologically dominant?

Q: Does PPP4R1 have a reproducible nuclear function through HDAC3 regulation, or is its best-supported role cytoplasmic signaling through PP4C?

Suggested Experiments

Experiment: Endogenous PPP4R1 and PPP4C co-immunoprecipitation after TNF stimulation, followed by phosphoproteomics in PPP4R1 knockout and rescue cells.

Hypothesis: PPP4R1 directs PP4C toward a limited set of NF-kappaB pathway substrates, including TRAF2/TRAF6 and IKK/NEMO-associated targets.

Type: phosphoproteomics

Experiment: Compare wild-type PPP4R1 rescue with PPP4C-binding-defective PPP4R1 mutants in NF-kappaB reporter, IL8/CCL20 secretion, and IKK phosphorylation assays.

Hypothesis: PPP4R1-dependent PP4C recruitment is required for negative regulation of canonical NF-kappaB signaling.

Type: cell-based pathway assay

Experiment: Subcellular fractionation and live-cell imaging of endogenously tagged PPP4R1 under basal, TNF-stimulated, and DNA replication stress conditions.

Hypothesis: PPP4R1 is primarily cytoplasmic during NF-kappaB regulation, with any nuclear/chromatin pool representing a context-dependent non-core function.

Type: localization assay

Deep Research

Falcon

(PPP4R1-deep-research-falcon.md)
this with annotations you find in gene/protein databases, but these can be outdated or inaccurate. Falcon Edison Scientific Literature 29 citations 2026-05-02T22:04:59.801370

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.

Comprehensive research report: human PPP4R1 (UniProt Q8TF05) – functional annotation

0) Target verification (critical disambiguation)

The requested target is the human gene PPP4R1 (a.k.a. PP4R1, also reported as regulatory subunit R1 of protein phosphatase 4). The literature in this report consistently uses PP4R1/PPP4R1 to denote a regulatory (non-catalytic) subunit of protein phosphatase 4 (PP4) that forms a complex with the PP4 catalytic subunit PPP4C (PP4c). This is distinct from other PP4 regulatory subunits (PPP4R2/PPP4R3/PPP4R4) that form alternate PP4 holoenzymes. (park2020functionalrolesof pages 1-3, yang2017theserinethreoninephosphatases pages 13-17)

1) Key concepts and current understanding

1.1 What PPP4R1 is (definition)

PPP4R1 is a regulatory/scaffolding subunit of the serine/threonine phosphatase PP4. PP4 holoenzymes are members of the PP2A-like phosphoprotein phosphatase family, in which a catalytic subunit associates with regulatory proteins that shape substrate selection, localization, and signaling outputs. In mammals, PP4 can form a heterodimer with PPP4R1 (PP4C/PP4R1) and other distinct assemblies with other regulatory subunits. (park2020functionalrolesof pages 1-3)

A foundational proteomics analysis of human PP4 complexes reported mutually exclusive PP4C assemblies that include a binary PP4C–PPP4R1 complex as one major form, emphasizing that PPP4R1 defines a specific PP4 holoenzyme class rather than being a generic interactor. (gingras2005anovelevolutionarily media 59a70f55, gingras2005anovelevolutionarily media 0cab0373)

1.2 Domain architecture and inferred molecular role

Evidence supports that PPP4R1 is a repeat-rich scaffold protein with PP2A-A-like HEAT repeats (often discussed as ARM/HEAT-type repeats in the broader literature), consistent with a regulatory subunit that presents binding surfaces for catalytic subunit and substrates/adaptors rather than catalyzing reactions itself. A review of serine/threonine phosphatases notes that PPP4R1 contains HEAT repeats similar to PP2A structural subunits and that PPP4R1 can form a heterodimeric complex with PPP4C. (yang2017theserinethreoninephosphatases pages 13-17)

Historically, biochemical fractionation of PP4-containing complexes identified a ~105 kDa PP4-associated protein with sequence similarity to the repeat region of the PP2A A (PR65) subunit, consistent with the later understanding of a PP2A-A-like repeat scaffold in the PP4 system (which aligns with the general properties expected for PPP4R1). (hastie2000anovel50 pages 9-10)

1.3 Catalytic function: what reaction is catalyzed, and what PPP4R1 contributes

PPP4R1 itself is not an enzyme; the catalytic activity resides in PPP4C, which hydrolyzes phosphate esters on phosphoserine/phosphothreonine residues of protein substrates. PPP4R1’s functional contribution is to form a PPP4C–PPP4R1 holoenzyme that can direct PP4 dephosphorylation activity toward specific signaling modules.

2) Pathways and biological processes supported by evidence

2.1 NF-κB pathway suppression (best-supported PPP4R1-specific function)

The strongest and most PPP4R1-specific mechanistic evidence in the retrieved corpus links PPP4R1-containing PP4 to negative regulation of NF-κB signaling, centered on the IKK complex and upstream adaptor/E3 ligases.

TRAF2/TRAF6 targeting: A primary study reported that PP4R1 interacts with TRAF2 (initially identified by yeast two-hybrid) and also with TRAF6 in a RING-domain dependent manner. Functionally, PP4R1 expression inhibited NF-κB activation driven by TRAF2/TRAF6 and upstream stimuli (e.g., TNF, EBV LMP1), while PP4R1 knockdown enhanced inflammatory outputs (e.g., IL8 induction). Mechanistically, PP4R1 mediated TRAF2 Ser11 dephosphorylation and reduced TRAF6 polyubiquitination, consistent with suppression of NF-κB activation at an early signaling node. (hadweh2014thepp4r1subunit pages 1-2)

IKK/NEMO bridging and viral immune evasion: In the context of Merkel polyomavirus small T antigen (tAg), PP4R1 was shown to form a complex with PP4c and to be required to bridge viral tAg to NEMO, enabling deactivation of the NF-κB pathway. PP4R1 depletion prevented tAg-mediated NF-κB inhibition and reduced suppression of pro-inflammatory cytokine production, demonstrating PPP4R1 is functionally required for this PP4-dependent NF-κB regulatory mechanism. (abdulsada2017thepp4r1subunit pages 1-2)

2024 mechanistic advance—AMBRA1 competition model in intestinal inflammation: A 2024 Cell Death & Differentiation study extends this axis into inflammatory disease biology. It reports that PP4R1 interacts with PP4c and references the known mechanism in which PP4R1 bridges IKK to PP4c to promote IKK dephosphorylation/inactivation. The study provides evidence that AMBRA1 can bind PP4R1 and PP4c to disrupt the PP4R1/PP4c–IKK module, thereby antagonizing IKK dephosphorylation, increasing IKK phosphorylation, and promoting intestinal inflammation. This positions the PP4R1/PP4c–IKK node as a regulatory checkpoint in inflammatory signaling with potential therapeutic implications. (xu2024ambra1promotesintestinal pages 1-3)

Expert synthesis: An authoritative PP4 review summarizes that a PP4C–PP4R1 complex can inactivate IKK via dephosphorylation, thereby preventing downstream NF-κB activation. (park2020functionalrolesof pages 7-8)

2.2 DNA damage response (DDR): strong for PP4 generally; weaker PPP4R1 attribution

Multiple authoritative reviews describe PP4 as a regulator of DDR, including dephosphorylation of substrates such as γ-H2AX, RPA2, KAP1, and 53BP1, which can influence checkpoint recovery, homologous recombination, and chromatin dynamics. However, within the evidence retrieved here, these DDR substrate assignments are most often attributed to PP4 complexes broadly or to PP4R2/PP4R3-containing assemblies rather than being conclusively mapped to the PPP4R1-containing heterodimer. Thus, DDR can be included as a plausible broader PP4 functional context but should be treated as indirect for PPP4R1 unless additional PPP4R1-specific DDR data are introduced. (park2020functionalrolesof pages 3-4, park2020functionalrolesof pages 1-3, ramos2019roleofprotein pages 5-6)

2.3 Chromatin-linked regulation via HDAC3

A DDR-focused review reports that Ppp4-R1 decreases HDAC3 activity through dephosphorylation of Ser424, linking PPP4R1-containing PP4 activity to chromatin regulation (via histone deacetylase control). This is one of the more specific substrate-level statements involving a PPP4R1-defined PP4 complex in the retrieved evidence, although it is presented in review form rather than as primary experimental text in this run. (ramos2019roleofprotein pages 5-6)

3) Subcellular localization

Direct PPP4R1 localization evidence in the retrieved corpus is limited compared with pathway evidence. Early PP4 complex work explicitly noted that the subcellular location of PPP4R1 had not been clearly established at that time (contrasting with centrosome-enriched PP4R2-associated assemblies). (hastie2000anovel50 pages 9-10)

Nonetheless, the PP4 complex architecture literature emphasizes that regulatory subunits determine subcellular targeting and that PP4 complexes can operate across compartments; the PPP4R1-defined PP4C assembly is one of the major cellular PP4C complexes. (park2020functionalrolesof pages 1-3, gingras2005anovelevolutionarily media 59a70f55)

4) Recent developments (prioritizing 2023–2024)

4.1 2024: PPP4R1/PP4c as an inflammation control point (IBD-relevant mechanism)

The 2024 Xu et al. study provides a current mechanistic model: AMBRA1 competes for PP4R1 and PP4c binding, disrupting PP4R1/PP4c-mediated IKK dephosphorylation and thereby enhancing NF-κB signaling and intestinal inflammation. The work links this signaling logic to therapeutic response context (reported improvement of infliximab therapy upon AMBRA1 deletion in the experimental system described). (xu2024ambra1promotesintestinal pages 1-3)

4.2 2024: PPP4R1 as a cancer biomarker candidate (LIHC/pan-cancer analytics)

A 2024 Translational Cancer Research paper (LIHC-focused) reported that PPP4R1 is overexpressed in cancer tissues versus adjacent tissues (including experimental verification of higher PPP4R1 protein in tumor vs paracancerous tissue in LIHC) and proposed clinical utility: diagnostic significance for 14 tumors with AUC > 0.7, prognostic associations in five tumor types, and PPP4R1 as an independent prognostic factor in LIHC (P < 0.05). It also reported a positive correlation between PPP4R1 expression and fludarabine IC50, suggesting potential relevance to drug sensitivity/resistance. (li2024thediagnosticprognostic pages 1-2)

5) Current applications and real-world implementations

5.1 Potential therapeutic leverage: PP4R1/PP4c–IKK node in inflammatory disease

The 2024 AMBRA1–PP4R1/PP4c mechanism supports a therapeutic concept: modulating the PP4R1/PP4c–IKK dephosphorylation axis could tune NF-κB-driven inflammation. While not yet a clinical intervention directed at PPP4R1, this is a concrete disease-proximal mechanism with treatment-response framing (infliximab) in a contemporary study. (xu2024ambra1promotesintestinal pages 1-3)

5.2 Biomarker development in oncology

The 2024 LIHC study positions PPP4R1 as a candidate diagnostic/prognostic biomarker and explores drug sensitivity correlations. Such analyses are currently most consistent with translational bioinformatics and validation workflows (e.g., ROC/AUC and survival modeling) rather than deployed clinical practice, but they represent the present state of “real-world implementation” efforts around PPP4R1. (li2024thediagnosticprognostic pages 1-2)

6) Expert opinions and authoritative synthesis

Authoritative reviews emphasize two points relevant to functional annotation:
1) Holoenzyme logic: PP4’s regulatory subunits (including PPP4R1) define function by determining target substrates and complex composition (heterodimers vs heterotrimers). (park2020functionalrolesof pages 1-3)
2) Signal integration: PP4 is repeatedly described as participating in multiple critical pathways (DDR, immune/NF-κB signaling, metabolism), and PPP4R1-containing PP4 is specifically represented as an NF-κB suppressor module through IKK regulation. (park2020functionalrolesof pages 7-8, park2020functionalrolesof pages 1-3)

7) Key statistics and quantitative findings (recent)

From LIHC/pan-cancer analyses (2024):
- PPP4R1 diagnostic significance reported for 14 tumors with ROC AUC > 0.7. (li2024thediagnosticprognostic pages 1-2)
- PPP4R1 identified as an independent prognostic factor in LIHC (P < 0.05, multivariable Cox regression reported). (li2024thediagnosticprognostic pages 1-2)
- PPP4R1 expression positively correlated with fludarabine IC50 (drug sensitivity association). (li2024thediagnosticprognostic pages 1-2)

From inflammatory signaling mechanism (2024):
- Mechanistic/phenotypic outcomes are presented as functional effects (e.g., antagonism of IKK dephosphorylation; increased inflammatory signaling; improved infliximab response upon AMBRA1 deletion), though specific numeric effect sizes are not extractable from the current evidence snippets in this run. (xu2024ambra1promotesintestinal pages 1-3)

8) Evidence-backed model summary (functional annotation)

PPP4R1 encodes a HEAT-repeat scaffold regulatory subunit that forms a PP4C–PPP4R1 holoenzyme. The best-supported direct biological function of this holoenzyme is negative regulation of inflammatory NF-κB signaling, mediated through interactions with upstream adaptors (TRAF2/TRAF6) and the IKK/NEMO axis, and modulated by competitive binding partners such as AMBRA1 (a 2024 mechanistic advance). Evidence for PPP4’s broader roles in DNA damage responses is strong at the PP4-complex level, but PPP4R1-specific DDR substrate assignment is less definitive in the retrieved sources and should be treated cautiously. (hadweh2014thepp4r1subunit pages 1-2, xu2024ambra1promotesintestinal pages 1-3, abdulsada2017thepp4r1subunit pages 1-2, park2020functionalrolesof pages 3-4)

9) Key figure (PP4 complex architecture)

A foundational schematic of human PP4C complexes (including the PP4C–PPP4R1 binary complex and other mutually exclusive PP4 assemblies) is available from Gingras et al. 2005 and supports the complex-composition framework used in this report. (gingras2005anovelevolutionarily media 59a70f55, gingras2005anovelevolutionarily media 0cab0373)

10) Summary table of evidence

Aspect Key finding Evidence type Representative source with year URL PaperQA citation id
Identity/complex PPP4R1 (PP4R1/MEG1) is the human regulatory subunit 1 of protein phosphatase 4 and forms a heterodimeric PP4 holoenzyme with catalytic PPP4C/PP4c; reviews distinguish this PP4C–PPP4R1 complex from PP4R2/PP4R3-containing heterotrimers. Review + primary Park & Lee 2020; Yang & Arrizabalaga 2017 https://doi.org/10.5483/bmbrep.2020.53.4.019 ; https://doi.org/10.1111/mmi.13715 (park2020functionalrolesof pages 1-3, yang2017theserinethreoninephosphatases pages 13-17)
Identity/complex Foundational proteomics mapped PP4C into mutually exclusive complexes, including a binary PP4C–PPP4R1 complex and the PP4cs complex with PP4R2/PP4R3, establishing core architecture for human PP4 assemblies. Primary Gingras et al. 2005 https://doi.org/10.1074/mcp.m500231-mcp200 (gingras2005anovelevolutionarily media 59a70f55)
Domains PPP4R1 has PP2A-A-like HEAT repeats/ARM-like architecture, consistent with a scaffold/adaptor role rather than catalytic activity. Review Yang & Arrizabalaga 2017 https://doi.org/10.1111/mmi.13715 (yang2017theserinethreoninephosphatases pages 13-17)
Domains A ~105 kDa PP4-associated protein with sequence similarity to repeats in the PP2A A/PR65 subunit was identified early in PP4 fractionation studies, supporting the long-repeat scaffold nature later assigned to PPP4R1. Primary Hastie et al. 2000 https://doi.org/10.1042/bj3470845 (hastie2000anovel50 pages 9-10)
Pathways/substrates PP4 complexes broadly regulate DNA-damage signaling by dephosphorylating substrates including γ-H2AX, RPA2, KAP1, and 53BP1; however, many of these assignments are strongest for PP4 holoenzymes generally or PP4R2/PP4R3-containing complexes, not always specifically PPP4R1-directed. Review Ramos et al. 2019; Park & Lee 2020 https://doi.org/10.15698/cst2019.03.178 ; https://doi.org/10.5483/bmbrep.2020.53.4.019 (ramos2019roleofprotein pages 5-6, park2020functionalrolesof pages 3-4)
Pathways/substrates PPP4R1-containing PP4 directly suppresses NF-κB by targeting the IKK axis; PP4R1 bridges PP4c to IKK/NEMO and is required for dephosphorylation-dependent inactivation of the complex. Primary Abdul-Sada et al. 2017 https://doi.org/10.18632/oncotarget.15836 (abdulsada2017thepp4r1subunit pages 1-2)
Pathways/substrates PPP4R1 also targets TRAF2 and TRAF6 to inhibit NF-κB activation, including TRAF2 Ser11 dephosphorylation and reduced TRAF6 polyubiquitination, linking the subunit to upstream inflammatory signal dampening. Primary Hadweh et al. 2014 https://doi.org/10.1016/j.cellsig.2014.08.001 (hadweh2014thepp4r1subunit pages 1-2)
Pathways/substrates A key 2024 advance showed AMBRA1 promotes intestinal inflammation by antagonizing PP4R1/PP4c-mediated IKK dephosphorylation; AMBRA1 competitively binds PP4R1 and PP4c, disrupts the PP4R1–PP4c–IKK module, and increases NF-κB signaling. Primary Xu et al. 2024 https://doi.org/10.1038/s41418-024-01275-9 (xu2024ambra1promotesintestinal pages 1-3)
Pathways/substrates PPP4R1-containing PP4 can also regulate chromatin-associated signaling outside canonical NF-κB, including decreased HDAC3 activity via dephosphorylation of HDAC3 Ser424. Review Ramos et al. 2019 https://doi.org/10.15698/cst2019.03.178 (ramos2019roleofprotein pages 5-6)
Localization Direct localization data for human PPP4R1 are comparatively sparse; available evidence indicates PP4 regulatory subunits help determine holoenzyme subcellular localization, and PPP4R1 has been reported as present in both cytoplasm and nucleus rather than a strictly compartment-restricted factor. Primary/review Chen et al. 2008; general PP4 reviews https://doi.org/10.1074/jbc.m803443200 ; https://doi.org/10.5483/bmbrep.2020.53.4.019 (park2020functionalrolesof pages 1-3)
Localization Earlier PP4 work noted that, unlike centrosomal PPP4R2, the subcellular location of PPP4R1 had not yet been clearly established, underscoring a persistent evidence gap in precise compartment-specific annotation. Primary Hastie et al. 2000 https://doi.org/10.1042/bj3470845 (hastie2000anovel50 pages 9-10)
Disease/application PPP4R1 is increasingly studied as a disease-relevant signaling regulator: inflammatory bowel disease data in 2024 position the PP4R1/PP4c–IKK node as a potential therapeutic leverage point, with AMBRA1 loss reducing pro-inflammatory cytokines and improving infliximab response in the reported model. Primary Xu et al. 2024 https://doi.org/10.1038/s41418-024-01275-9 (xu2024ambra1promotesintestinal pages 1-3)
Disease/application A 2024 LIHC study reported PPP4R1 overexpression in tumor tissue, diagnostic value across 14 tumors with AUC >0.7, prognostic significance in five tumors, independent prognostic value in LIHC (P<0.05), and positive correlation with fludarabine IC50, supporting biomarker potential though mainly from bioinformatic/validation analyses. Primary + database-style bioinformatics Li et al. 2024 https://doi.org/10.21037/tcr-23-1744 (li2024thediagnosticprognostic pages 1-2)
Disease/application Open Targets lists current, relatively low-to-moderate evidence disease associations for PPP4R1 including Alzheimer disease, multiple sclerosis, neurodegenerative disease, smoking initiation, and mathematical ability; these are hypothesis-generating rather than definitive functional annotations. Database Open Targets search (current platform result) https://platform.opentargets.org (li2024thediagnosticprognostic pages 1-2)

Table: This table summarizes verified functional-annotation evidence for human PPP4R1/PP4R1 (UniProt Q8TF05), emphasizing recent 2024 studies and foundational PP4 complex architecture papers. It highlights what is well supported, where evidence is indirect, and where localization or substrate specificity remains less resolved.

References (URLs and publication dates)

  • Xu W. et al. AMBRA1 promotes intestinal inflammation by antagonizing PP4R1/PP4c mediated IKK dephosphorylation. Cell Death & Differentiation (Feb 2024). https://doi.org/10.1038/s41418-024-01275-9 (xu2024ambra1promotesintestinal pages 1-3)
  • Li X. et al. Diagnostic/prognostic/drug sensitivity analysis of PPP4R1 in LIHC. Translational Cancer Research (Feb 2024). https://doi.org/10.21037/tcr-23-1744 (li2024thediagnosticprognostic pages 1-2)
  • Hadweh P. et al. PP4R1 targets TRAF2/TRAF6 to inhibit NF-κB activation. Cellular Signalling (Dec 2014). https://doi.org/10.1016/j.cellsig.2014.08.001 (hadweh2014thepp4r1subunit pages 1-2)
  • Abdul-Sada H. et al. PP4R1 is essential for inhibition of NF-κB by Merkel polyomavirus small tumor antigen. Oncotarget (Mar 2017). https://doi.org/10.18632/oncotarget.15836 (abdulsada2017thepp4r1subunit pages 1-2)
  • Yang C., Arrizabalaga G. Serine/threonine phosphatases of apicomplexan parasites (contains specific statements about human PPP4R1 HEAT repeats and PP4C heterodimer formation). Molecular Microbiology (Oct 2017). https://doi.org/10.1111/mmi.13715 (yang2017theserinethreoninephosphatases pages 13-17)
  • Park J., Lee D.-H. Functional roles of PP4. BMB Reports (Apr 2020). https://doi.org/10.5483/bmbrep.2020.53.4.019 (park2020functionalrolesof pages 1-3)
  • Ramos F. et al. PP1/PP2A/PP4 roles in DNA damage response. Cell Stress (Mar 2019). https://doi.org/10.15698/cst2019.03.178 (ramos2019roleofprotein pages 5-6)
  • Campos A., Clemente-Blanco A. Protein phosphatases in DDR. Int. J. Mol. Sci. (Jan 2020). https://doi.org/10.3390/ijms21020446 (campos2020cellcycleand pages 6-8)
  • Gingras A.-C. et al. PP4 complex architecture and cisplatin sensitivity. Molecular & Cellular Proteomics (Nov 2005). https://doi.org/10.1074/mcp.m500231-mcp200 (gingras2005anovelevolutionarily media 59a70f55)
  • Hastie C.J. et al. PP4 complexes and early evidence of PP2A-A-like repeats in a PP4-associated ~105 kDa factor. Biochemical Journal (May 2000). https://doi.org/10.1042/bj3470845 (hastie2000anovel50 pages 9-10)

References

  1. (park2020functionalrolesof pages 1-3): Jaehong Park and Dong-Hyun Lee. Functional roles of protein phosphatase 4 in multiple aspects of cellular physiology: a friend and a foe. BMB Reports, 53:181-190, Apr 2020. URL: https://doi.org/10.5483/bmbrep.2020.53.4.019, doi:10.5483/bmbrep.2020.53.4.019. This article has 52 citations and is from a peer-reviewed journal.

  2. (yang2017theserinethreoninephosphatases pages 13-17): Chunlin Yang and Gustavo Arrizabalaga. The serine/threonine phosphatases of apicomplexan parasites. Molecular Microbiology, 106:1-21, Oct 2017. URL: https://doi.org/10.1111/mmi.13715, doi:10.1111/mmi.13715. This article has 53 citations and is from a domain leading peer-reviewed journal.

  3. (gingras2005anovelevolutionarily media 59a70f55): Anne-Claude Gingras, Michael Caballero, Marcel Zarske, Amy Sanchez, Tony R. Hazbun, Stanley Fields, Nahum Sonenberg, Ernst Hafen, Brian Raught, and Ruedi Aebersold. A novel, evolutionarily conserved protein phosphatase complex involved in cisplatin sensitivity. Molecular & Cellular Proteomics, 4:1725-1740, Nov 2005. URL: https://doi.org/10.1074/mcp.m500231-mcp200, doi:10.1074/mcp.m500231-mcp200. This article has 236 citations and is from a domain leading peer-reviewed journal.

  4. (gingras2005anovelevolutionarily media 0cab0373): Anne-Claude Gingras, Michael Caballero, Marcel Zarske, Amy Sanchez, Tony R. Hazbun, Stanley Fields, Nahum Sonenberg, Ernst Hafen, Brian Raught, and Ruedi Aebersold. A novel, evolutionarily conserved protein phosphatase complex involved in cisplatin sensitivity. Molecular & Cellular Proteomics, 4:1725-1740, Nov 2005. URL: https://doi.org/10.1074/mcp.m500231-mcp200, doi:10.1074/mcp.m500231-mcp200. This article has 236 citations and is from a domain leading peer-reviewed journal.

  5. (hastie2000anovel50 pages 9-10): C. James HASTIE, Graeme K. CARNEGIE, Nick MORRICE, and Patricia T. W. COHEN. A novel 50 kda protein forms complexes with protein phosphatase 4 and is located at centrosomal microtubule organizing centres. The Biochemical journal, 347 Pt 3:845-55, May 2000. URL: https://doi.org/10.1042/bj3470845, doi:10.1042/bj3470845. This article has 95 citations.

  6. (hadweh2014thepp4r1subunit pages 1-2): Paul Hadweh, Hasem Habelhah, Elliott Kieff, George Mosialos, and Eudoxia Hatzivassiliou. The pp4r1 subunit of protein phosphatase pp4 targets traf2 and traf6 to mediate inhibition of nf-κb activation. Cellular signalling, 26 12:2730-7, Dec 2014. URL: https://doi.org/10.1016/j.cellsig.2014.08.001, doi:10.1016/j.cellsig.2014.08.001. This article has 32 citations and is from a peer-reviewed journal.

  7. (abdulsada2017thepp4r1subunit pages 1-2): Hussein Abdul-Sada, Marietta Müller, Rajni Mehta, Rachel Toth, J. Simon C. Arthur, Adrian Whitehouse, and Andrew Macdonald. The pp4r1 sub-unit of protein phosphatase pp4 is essential for inhibition of nf-κb by merkel polyomavirus small tumour antigen. Oncotarget, 8:25418-25432, Mar 2017. URL: https://doi.org/10.18632/oncotarget.15836, doi:10.18632/oncotarget.15836. This article has 53 citations.

  8. (xu2024ambra1promotesintestinal pages 1-3): Weimin Xu, Zhebin Hua, Yaosheng Wang, Wenbo Tang, Weijun Ou, Fangyuan Liu, Yiqing Yang, Wenjun Ding, Zhongchuan Wang, Long Cui, Wensong Ge, Yubei Gu, Xiaolei Wang, YingWei Chen, Chen-Ying Liu, and Peng Du. Ambra1 promotes intestinal inflammation by antagonizing pp4r1/pp4c mediated ikk dephosphorylation in an autophagy-independent manner. Cell death and differentiation, 31:618-634, Feb 2024. URL: https://doi.org/10.1038/s41418-024-01275-9, doi:10.1038/s41418-024-01275-9. This article has 11 citations and is from a domain leading peer-reviewed journal.

  9. (park2020functionalrolesof pages 7-8): Jaehong Park and Dong-Hyun Lee. Functional roles of protein phosphatase 4 in multiple aspects of cellular physiology: a friend and a foe. BMB Reports, 53:181-190, Apr 2020. URL: https://doi.org/10.5483/bmbrep.2020.53.4.019, doi:10.5483/bmbrep.2020.53.4.019. This article has 52 citations and is from a peer-reviewed journal.

  10. (park2020functionalrolesof pages 3-4): Jaehong Park and Dong-Hyun Lee. Functional roles of protein phosphatase 4 in multiple aspects of cellular physiology: a friend and a foe. BMB Reports, 53:181-190, Apr 2020. URL: https://doi.org/10.5483/bmbrep.2020.53.4.019, doi:10.5483/bmbrep.2020.53.4.019. This article has 52 citations and is from a peer-reviewed journal.

  11. (ramos2019roleofprotein pages 5-6): Facundo Ramos, María Teresa Villoria, Esmeralda Alonso-Rodríguez, and Andrés Clemente-Blanco. Role of protein phosphatases pp1, pp2a, pp4 and cdc14 in the dna damage response. Cell Stress, 3:70-85, Mar 2019. URL: https://doi.org/10.15698/cst2019.03.178, doi:10.15698/cst2019.03.178. This article has 77 citations.

  12. (li2024thediagnosticprognostic pages 1-2): Xiaowei Li, Yinglian Pan, Siren Feng, Weimei Xing, Bo Lin, Wei Li, Mengsen Li, and Mingyue Zhu. The diagnostic, prognostic, drug sensitivity and cerna internet of ppp4r1 in liver hepatocellular carcinoma (lihc). Translational Cancer Research, 13:594-612, Feb 2024. URL: https://doi.org/10.21037/tcr-23-1744, doi:10.21037/tcr-23-1744. This article has 3 citations.

  13. (campos2020cellcycleand pages 6-8): Adrián Campos and Andrés Clemente-Blanco. Cell cycle and dna repair regulation in the damage response: protein phosphatases take over the reins. International Journal of Molecular Sciences, 21:446, Jan 2020. URL: https://doi.org/10.3390/ijms21020446, doi:10.3390/ijms21020446. This article has 126 citations.

Citations

  1. park2020functionalrolesof pages 1-3
  2. yang2017theserinethreoninephosphatases pages 13-17
  3. park2020functionalrolesof pages 7-8
  4. ramos2019roleofprotein pages 5-6
  5. li2024thediagnosticprognostic pages 1-2
  6. campos2020cellcycleand pages 6-8
  7. park2020functionalrolesof pages 3-4
  8. https://doi.org/10.5483/bmbrep.2020.53.4.019
  9. https://doi.org/10.1111/mmi.13715
  10. https://doi.org/10.1074/mcp.m500231-mcp200
  11. https://doi.org/10.1042/bj3470845
  12. https://doi.org/10.15698/cst2019.03.178
  13. https://doi.org/10.18632/oncotarget.15836
  14. https://doi.org/10.1016/j.cellsig.2014.08.001
  15. https://doi.org/10.1038/s41418-024-01275-9
  16. https://doi.org/10.1074/jbc.m803443200
  17. https://doi.org/10.21037/tcr-23-1744
  18. https://platform.opentargets.org
  19. https://doi.org/10.3390/ijms21020446
  20. https://doi.org/10.5483/bmbrep.2020.53.4.019,
  21. https://doi.org/10.1111/mmi.13715,
  22. https://doi.org/10.1074/mcp.m500231-mcp200,
  23. https://doi.org/10.1042/bj3470845,
  24. https://doi.org/10.1016/j.cellsig.2014.08.001,
  25. https://doi.org/10.18632/oncotarget.15836,
  26. https://doi.org/10.1038/s41418-024-01275-9,
  27. https://doi.org/10.15698/cst2019.03.178,
  28. https://doi.org/10.21037/tcr-23-1744,
  29. https://doi.org/10.3390/ijms21020446,

📄 View Raw YAML

id: Q8TF05
gene_symbol: PPP4R1
product_type: PROTEIN
status: COMPLETE
taxon:
  id: NCBITaxon:9606
  label: Homo sapiens
description: >-
  PPP4R1 encodes PP4 regulatory subunit 1, a HEAT/ARM-repeat scaffolding
  subunit of the serine/threonine protein phosphatase 4 holoenzyme. PPP4R1
  binds the catalytic subunit PPP4C to form a PP4C-PPP4R1 complex that directs
  phosphatase activity toward selected targets. The best-supported
  PPP4R1-specific process is dampening canonical NF-kappaB signaling through
  PP4-dependent regulation of TRAF2/TRAF6 and the IKK/NEMO axis. Broader PP4
  roles in DNA damage response are well established for PP4 complexes, but the
  strongest DDR substrate evidence is not specific to the PPP4R1-containing
  holoenzyme.
alternative_products:
  - name: 1 (PP4Rmeg)
    id: Q8TF05-1
  - name: '2'
    id: Q8TF05-2
    sequence_note: VSP_009469
existing_annotations:
  - term:
      id: GO:0005737
      label: cytoplasm
    qualifier: is_active_in
    evidence_type: IBA
    original_reference_id: GO_REF:0000033
    review:
      summary: >-
        Cytoplasmic localization is consistent with PPP4R1 acting in PP4
        signaling complexes, although precise compartment-specific localization
        is not strongly resolved.
      action: ACCEPT
      reason: >-
        Falcon research notes sparse direct localization evidence but supports
        cytoplasm as a reasonable broad location for PPP4R1-containing PP4
        signaling complexes.
      supported_by:
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            Direct localization data for human PPP4R1 are comparatively sparse;
            available evidence indicates PP4 regulatory subunits help determine
            holoenzyme subcellular localization.
  - term:
      id: GO:0019888
      label: protein phosphatase regulator activity
    qualifier: enables
    evidence_type: IBA
    original_reference_id: GO_REF:0000033
    review:
      summary: >-
        PPP4R1 is a non-catalytic regulatory/scaffolding subunit of PP4 that
        binds PPP4C and helps define holoenzyme substrate targeting.
      action: ACCEPT
      reason: >-
        This is the most appropriate molecular-function annotation for PPP4R1:
        it regulates a protein phosphatase rather than catalyzing
        dephosphorylation itself.
      supported_by:
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1 is a regulatory/scaffolding subunit of the serine/threonine
            phosphatase PP4.
        - reference_id: PMID:10026142
          supporting_text: >-
            The PP4R1 cDNA clone engineered with an N-terminal Myc tag was
            expressed in COS M6 cells and PP4C co-immunoprecipitated with
            Myc-tagged PP4R1.
  - term:
      id: GO:0005515
      label: protein binding
    qualifier: enables
    evidence_type: IPI
    original_reference_id: PMID:16085932
    review:
      summary: >-
        This IPI annotation captures PPP4R1 binding to PPP4C, but generic
        protein binding is less informative than the known PP4 regulatory
        subunit activity.
      action: MODIFY
      reason: >-
        PPP4R1's PPP4C interaction should be represented as protein phosphatase
        regulator activity rather than the uninformative protein binding term.
      proposed_replacement_terms:
        - id: GO:0019888
          label: protein phosphatase regulator activity
      supported_by:
        - reference_id: PMID:16085932
          supporting_text: >-
            Using a combination of tandem affinity purification tagging and mass
            spectrometry, we characterized a novel, evolutionarily conserved
            protein phosphatase 4 (PP4)-containing complex.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            A foundational proteomics analysis of human PP4 complexes reported
            mutually exclusive PP4C assemblies that include a binary
            PP4C-PPP4R1 complex.
  - term:
      id: GO:0005515
      label: protein binding
    qualifier: enables
    evidence_type: IPI
    original_reference_id: PMID:17353931
    review:
      summary: >-
        This high-throughput interactome annotation reports PPP4C binding, but
        the biologically meaningful interpretation is PPP4 regulator/scaffold
        activity.
      action: MODIFY
      reason: >-
        Replace generic protein binding with the more informative protein
        phosphatase regulator activity term supported by the PPP4R1-PPP4C
        complex literature.
      proposed_replacement_terms:
        - id: GO:0019888
          label: protein phosphatase regulator activity
      supported_by:
        - reference_id: PMID:17353931
          supporting_text: >-
            Mapping protein-protein interactions is an invaluable tool for
            understanding protein function.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1 defines a specific PP4 holoenzyme class rather than being a
            generic interactor.
  - term:
      id: GO:0005515
      label: protein binding
    qualifier: enables
    evidence_type: IPI
    original_reference_id: PMID:18614045
    review:
      summary: >-
        This interaction entry concerns PP4 complex biology, but the cited
        gamma-H2AX paper primarily supports a PP4R2/PP4R3-containing complex
        rather than a PPP4R1-specific DDR role.
      action: REMOVE
      reason: >-
        The local publication text supports a PP4C/PP4R2/PP4R3beta gamma-H2AX
        phosphatase complex rather than a PPP4R1-containing complex, so this
        PMID should not support a PPP4R1 functional annotation.
      supported_by:
        - reference_id: PMID:18614045
          supporting_text: >-
            Here we describe a three-protein PP4 phosphatase complex in
            mammalian cells, containing PP4C, PP4R2, and PP4R3beta, that
            specifically dephosphorylates ATR-mediated gamma-H2AX.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            DDR substrate assignments are most often attributed to PP4
            complexes broadly or to PP4R2/PP4R3-containing assemblies rather
            than being conclusively mapped to the PPP4R1-containing heterodimer.
  - term:
      id: GO:0005515
      label: protein binding
    qualifier: enables
    evidence_type: IPI
    original_reference_id: PMID:18715871
    review:
      summary: >-
        This PP4 regulatory-subunit study distinguishes PP4R4 from PP4R1
        complexes; the PPP4R1-PPP4C interaction should still be represented by
        the regulator activity term rather than protein binding.
      action: MODIFY
      reason: >-
        Generic protein binding does not capture the role of PPP4R1 as a PP4
        regulatory/scaffolding subunit.
      proposed_replacement_terms:
        - id: GO:0019888
          label: protein phosphatase regulator activity
      supported_by:
        - reference_id: PMID:18715871
          supporting_text: >-
            PP4c interacts with regulatory proteins, which specify substrate
            targeting and intracellular localization.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PP4 holoenzymes are members of the PP2A-like phosphoprotein
            phosphatase family, in which a catalytic subunit associates with
            regulatory proteins that shape substrate selection, localization,
            and signaling outputs.
  - term:
      id: GO:0005515
      label: protein binding
    qualifier: enables
    evidence_type: IPI
    original_reference_id: PMID:26496610
    review:
      summary: >-
        This quantitative interactome annotation is compatible with PPP4R1
        interacting with PPP4C, but protein binding is not the best GO
        representation of the established function.
      action: MODIFY
      reason: >-
        Replace with protein phosphatase regulator activity to capture the
        regulatory-subunit role.
      proposed_replacement_terms:
        - id: GO:0019888
          label: protein phosphatase regulator activity
      supported_by:
        - reference_id: PMID:26496610
          supporting_text: >-
            Using quantitative proteomics, we detect specific interactions,
            estimate interaction stoichiometries, and measure cellular
            abundances of interacting proteins.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1 is a repeat-rich scaffold protein with PP2A-A-like HEAT
            repeats, consistent with a regulatory subunit that presents binding
            surfaces for catalytic subunit and substrates/adaptors.
  - term:
      id: GO:0005515
      label: protein binding
    qualifier: enables
    evidence_type: IPI
    original_reference_id: PMID:27880917
    review:
      summary: >-
        The phosphatase interactome result is consistent with PP4 complex
        membership, but the actionable GO annotation should be PPP4R1's
        phosphatase regulator role.
      action: MODIFY
      reason: >-
        PPP4R1 is not merely a binding protein; it is the regulatory/scaffolding
        subunit of a PP4 holoenzyme.
      proposed_replacement_terms:
        - id: GO:0019888
          label: protein phosphatase regulator activity
      supported_by:
        - reference_id: PMID:27880917
          supporting_text: >-
            We identified 1,335 high-confidence interactions (1,104 previously
            unreported), implicating these phosphatases in the regulation of a
            variety of cellular processes.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1's functional contribution is to form a PPP4C-PPP4R1
            holoenzyme that can direct PP4 dephosphorylation activity toward
            specific signaling modules.
  - term:
      id: GO:0005515
      label: protein binding
    qualifier: enables
    evidence_type: IPI
    original_reference_id: PMID:33961781
    review:
      summary: >-
        This proteome-scale interaction supports PPP4C association but is still
        too generic as a protein binding annotation.
      action: MODIFY
      reason: >-
        The PPP4C interaction should be curated as protein phosphatase regulator
        activity in the PP4 complex context.
      proposed_replacement_terms:
        - id: GO:0019888
          label: protein phosphatase regulator activity
      supported_by:
        - reference_id: PMID:33961781
          supporting_text: >-
            Dual proteome-scale networks reveal cell-specific remodeling of the
            human interactome.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1 is a regulatory/scaffolding subunit of the serine/threonine
            phosphatase PP4.
  - term:
      id: GO:0005515
      label: protein binding
    qualifier: enables
    evidence_type: IPI
    original_reference_id: PMID:40205054
    review:
      summary: >-
        This recent multimodal cell-map interaction should not leave PPP4R1 with
        a generic protein binding function when the PP4 regulatory role is known.
      action: MODIFY
      reason: >-
        Use protein phosphatase regulator activity to capture the functional
        consequence of PPP4R1 binding PPP4C.
      proposed_replacement_terms:
        - id: GO:0019888
          label: protein phosphatase regulator activity
      supported_by:
        - reference_id: PMID:40205054
          supporting_text: >-
            Multimodal cell maps as a foundation for structural and functional
            genomics.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1 defines a specific PP4 holoenzyme class rather than being a
            generic interactor.
  - term:
      id: GO:0004721
      label: phosphoprotein phosphatase activity
    qualifier: contributes_to
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: >-
        This annotation is acceptable only with the contributes_to qualifier,
        but the broad phosphoprotein phosphatase term should be replaced with
        the more specific protein serine/threonine phosphatase activity term.
      action: MODIFY
      reason: >-
        PPP4R1 forms a complex with serine/threonine phosphatase PPP4C, so
        contributes_to protein serine/threonine phosphatase activity is
        defensible, while enables would be misleading.
      proposed_replacement_terms:
        - id: GO:0004722
          label: protein serine/threonine phosphatase activity
      supported_by:
        - reference_id: PMID:10026142
          supporting_text: >-
            These data indicate that one form of PP4 is similar to the core
            complex of PP2A in that it consists of a catalytic subunit and a
            PP2AA-like structural subunit.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1 itself is not an enzyme; the catalytic activity resides in
            PPP4C.
  - term:
      id: GO:0006468
      label: protein phosphorylation
    qualifier: involved_in
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: >-
        This is an opposite-reaction misannotation. PPP4R1 is a regulatory
        subunit of protein phosphatase 4, which removes phosphate groups from
        phosphoproteins rather than phosphorylating them.
      action: REMOVE
      reason: >-
        PPP4R1 is not a kinase, and the supported PP4 biology concerns
        dephosphorylation or regulation of phosphatase activity, not protein
        phosphorylation.
      supported_by:
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1 itself is not an enzyme; the catalytic activity resides in
            PPP4C, which hydrolyzes phosphate esters on phosphoserine/
            phosphothreonine residues.
  - term:
      id: GO:0030289
      label: protein phosphatase 4 complex
    qualifier: part_of
    evidence_type: ISS
    original_reference_id: GO_REF:0000024
    review:
      summary: >-
        PPP4R1 is a component of the PP4C-PPP4R1 protein phosphatase 4
        holoenzyme.
      action: ACCEPT
      reason: >-
        Multiple sources support PPP4R1 as a stable regulatory subunit in a
        PP4C-PPP4R1 complex.
      supported_by:
        - reference_id: PMID:10026142
          supporting_text: >-
            The final product contained two major proteins: the PP4 catalytic
            subunit plus a protein that migrated as a doublet of 120-125 kDa.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            In mammals, PP4 can form a heterodimer with PPP4R1 (PP4C/PP4R1)
            and other distinct assemblies with other regulatory subunits.
  - term:
      id: GO:0007165
      label: signal transduction
    qualifier: involved_in
    evidence_type: NAS
    original_reference_id: PMID:10026142
    review:
      summary: >-
        The broad signal transduction annotation should be replaced by the
        specific PPP4R1-supported process: negative regulation of canonical
        NF-kappaB signal transduction.
      action: MODIFY
      reason: >-
        PPP4R1-specific pathway evidence supports inhibition of canonical
        NF-kappaB signaling through TRAF2/TRAF6 and IKK/NEMO, not generic signal
        transduction.
      proposed_replacement_terms:
        - id: GO:0043124
          label: negative regulation of canonical NF-kappaB signal transduction
      supported_by:
        - reference_id: PMID:25134449
          supporting_text: >-
            Exogenous expression of PP4R1 inhibited NF-kappaB activation by
            TRAF2, TRAF6, TNF and the Epstein-Barr virus oncoprotein LMP1.
        - reference_id: PMID:28445980
          supporting_text: >-
            Formation of a complex with PP4R1 and PP4c is required to bridge
            MCPyV tAg to the NEMO adaptor protein, allowing deactivation of the
            NF-kB pathway.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            The best-supported direct biological function of this holoenzyme is
            negative regulation of inflammatory NF-kappaB signaling.
  - term:
      id: GO:0019888
      label: protein phosphatase regulator activity
    qualifier: enables
    evidence_type: NAS
    original_reference_id: PMID:10026142
    review:
      summary: >-
        The founding biochemical study supports PPP4R1 as a PP4 regulatory
        subunit that binds PPP4C.
      action: ACCEPT
      reason: >-
        This is a direct, specific annotation for PPP4R1's core molecular
        function.
      supported_by:
        - reference_id: PMID:10026142
          supporting_text: >-
            Amino acid sequence information of several peptides derived from the
            105 kDa protein was utilized to isolate a human cDNA clone.
        - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
          supporting_text: >-
            PPP4R1 encodes a HEAT-repeat scaffold regulatory subunit that forms
            a PP4C-PPP4R1 holoenzyme.
references:
  - 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: PMID:10026142
    title: Purification and identification of a novel subunit of protein serine/threonine phosphatase 4.
    findings: []
  - id: PMID:11729228
    title: Cloning and characterization of a novel subunit of protein serine/threonine phosphatase 4 from mesangial cells.
    findings: []
  - id: PMID:15805470
    title: Histone deacetylase 3 (HDAC3) activity is regulated by interaction with protein serine/threonine phosphatase 4.
    findings: []
  - id: PMID:16085932
    title: A novel, evolutionarily conserved protein phosphatase complex involved in cisplatin sensitivity.
    findings: []
  - id: PMID:17353931
    title: Large-scale mapping of human protein-protein interactions by mass spectrometry.
    findings: []
  - id: PMID:18614045
    title: A PP4-phosphatase complex dephosphorylates gamma-H2AX generated during DNA replication.
    findings: []
  - id: PMID:18715871
    title: PP4R4/KIAA1622 forms a novel stable cytosolic complex with phosphoprotein phosphatase 4.
    findings: []
  - id: PMID:25134449
    title: The PP4R1 subunit of protein phosphatase PP4 targets TRAF2 and TRAF6 to mediate inhibition of NF-kappaB activation.
    findings: []
  - id: PMID:26496610
    title: A human interactome in three quantitative dimensions organized by stoichiometries and abundances.
    findings: []
  - id: PMID:27880917
    title: Phenotypic and Interaction Profiling of the Human Phosphatases Identifies Diverse Mitotic Regulators.
    findings: []
  - id: PMID:28445980
    title: The PP4R1 sub-unit of protein phosphatase PP4 is essential for inhibition of NF-kappaB by merkel polyomavirus small tumour antigen.
    findings: []
  - id: PMID:33961781
    title: Dual proteome-scale networks reveal cell-specific remodeling of the human interactome.
    findings: []
  - id: PMID:40205054
    title: Multimodal cell maps as a foundation for structural and functional genomics.
    findings: []
  - id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
    title: Falcon deep research report for human PPP4R1
    findings: []
core_functions:
  - description: >-
      Regulatory/scaffolding subunit of the PP4C-PPP4R1 serine/threonine
      phosphatase holoenzyme that contributes to phosphoprotein phosphatase
      activity and directs PP4-dependent negative regulation of canonical
      NF-kappaB signaling.
    molecular_function:
      id: GO:0019888
      label: protein phosphatase regulator activity
    directly_involved_in:
      - id: GO:0043124
        label: negative regulation of canonical NF-kappaB signal transduction
    locations:
      - id: GO:0005737
        label: cytoplasm
    in_complex:
      id: GO:0030289
      label: protein phosphatase 4 complex
    supported_by:
      - reference_id: PMID:10026142
        supporting_text: >-
          PP4C co-immunoprecipitated with Myc-tagged PP4R1.
      - reference_id: PMID:25134449
        supporting_text: >-
          Exogenous expression of PP4R1 inhibited NF-kappaB activation by
          TRAF2, TRAF6, TNF and the Epstein-Barr virus oncoprotein LMP1.
      - reference_id: file:human/PPP4R1/PPP4R1-deep-research-falcon.md
        supporting_text: >-
          PPP4R1 encodes a HEAT-repeat scaffold regulatory subunit that forms a
          PP4C-PPP4R1 holoenzyme.
proposed_new_terms: []
suggested_questions:
  - question: Which endogenous human substrates are specifically directed by the PPP4R1-containing PP4 holoenzyme rather than by PP4R2/PP4R3 or PP4R4 complexes?
  - question: In which cell types is PPP4R1-dependent negative regulation of canonical NF-kappaB signaling physiologically dominant?
  - question: Does PPP4R1 have a reproducible nuclear function through HDAC3 regulation, or is its best-supported role cytoplasmic signaling through PP4C?
suggested_experiments:
  - description: Endogenous PPP4R1 and PPP4C co-immunoprecipitation after TNF stimulation, followed by phosphoproteomics in PPP4R1 knockout and rescue cells.
    experiment_type: phosphoproteomics
    hypothesis: PPP4R1 directs PP4C toward a limited set of NF-kappaB pathway substrates, including TRAF2/TRAF6 and IKK/NEMO-associated targets.
  - description: Compare wild-type PPP4R1 rescue with PPP4C-binding-defective PPP4R1 mutants in NF-kappaB reporter, IL8/CCL20 secretion, and IKK phosphorylation assays.
    experiment_type: cell-based pathway assay
    hypothesis: PPP4R1-dependent PP4C recruitment is required for negative regulation of canonical NF-kappaB signaling.
  - description: Subcellular fractionation and live-cell imaging of endogenously tagged PPP4R1 under basal, TNF-stimulated, and DNA replication stress conditions.
    experiment_type: localization assay
    hypothesis: PPP4R1 is primarily cytoplasmic during NF-kappaB regulation, with any nuclear/chromatin pool representing a context-dependent non-core function.