GADD45B

UniProt ID: O75293
Organism: Homo sapiens
Review Status: COMPLETE
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Gene Description

GADD45B (Growth arrest and DNA damage-inducible protein GADD45 beta, also known as MyD118) is a stress-inducible protein that mediates activation of stress-responsive MAPK signaling pathways. The protein binds directly to the N-terminal regulatory domain of MTK1/MEKK4 (MAP3K4), relieving autoinhibition and activating its kinase activity. This leads to downstream activation of both p38 MAPK and JNK cascades in response to environmental stresses including UV irradiation, genotoxic agents (MMS), and gamma irradiation. GADD45B also interacts with MKK7 (MAP2K7), where it blocks kinase activity and suppresses JNK-mediated apoptosis. This dual activity - activating MTK1/MEKK4 while inhibiting MKK7 - positions GADD45B as a key modulator of stress responses and cell fate decisions. The gene is transcriptionally regulated by NF-kB, and its expression is elevated in multiple myeloma where it promotes cancer cell survival by blocking MKK7/JNK-mediated apoptosis.

Existing Annotations Review

GO Term Evidence Action Reason
GO:0051726 regulation of cell cycle
IBA
GO_REF:0000033
KEEP AS NON CORE
Summary: The GADD45 family is known to regulate cell cycle through interaction with GADD45GIP1/CRIF1 which modulates Cdc2-cyclin B1 and Cdk2-cyclin E activity [PMID:12716909]. IBA evidence from phylogenetic inference is appropriate but this represents a secondary/downstream effect of GADD45B rather than its core molecular function.
Supporting Evidence:
PMID:12716909
Recombinant CRIF1 inhibits the histone H1 kinase activity of immunoprecipitated Cdc2-cyclin B1 and Cdk2-cyclin E, and the inhibitory effects were additive with Gadd45 proteins
GO:0005634 nucleus
IBA
GO_REF:0000033
ACCEPT
Summary: Nuclear localization is confirmed by direct experimental evidence [PMID:9827804]. IBA provides supporting phylogenetic evidence consistent with experimental data.
Supporting Evidence:
PMID:9827804
Using a yeast two-hybrid method, three related proteins, GADD45alpha (= GADD45), GADD45, (= MyD118), and GADD45gamma, were identified that bound to an N-terminal domain of MTK1
GO:0005737 cytoplasm
IBA
GO_REF:0000033
ACCEPT
Summary: Cytoplasmic localization is confirmed by direct experimental evidence [PMID:9827804]. IBA provides supporting phylogenetic evidence consistent with experimental data.
Supporting Evidence:
PMID:9827804
These proteins activated MTK1 kinase activity, both in vivo and in vitro
GO:0005634 nucleus
IEA
GO_REF:0000002
ACCEPT
Summary: Consistent with IDA-supported annotation from PMID:9827804. InterPro-based inference provides supporting automated evidence for nuclear localization.
GO:0006915 apoptotic process
IEA
GO_REF:0000043
MODIFY
Summary: GADD45B has a complex role in apoptosis. It can promote apoptosis via MTK1/MEKK4 activation leading to p38/JNK stress signaling [PMID:9827804], but also acts as an anti-apoptotic factor by inhibiting MKK7/JNK in cancer contexts [PMID:25314077]. The generic term 'apoptotic process' does not capture this complexity. Should be replaced with the more specific term matching the IDA annotation.
Supporting Evidence:
PMID:9827804
Expression of the GADD45-like genes induces p38/JNK activation and apoptosis, which can be partially suppressed by coexpression of a dominant inhibitory MTK1 mutant protein
PMID:25314077
GADD45Ξ² promotes the survival of MM cells by inhibiting JNK-mediated apoptosis
GO:0030154 cell differentiation
IEA
GO_REF:0000043
MARK AS OVER ANNOTATED
Summary: GADD45B (originally named MyD118 for myeloid differentiation primary response) was identified in myeloid differentiation studies. The keyword-based inference is plausible but lacks direct experimental support for GADD45B specifically being required for differentiation. This may be an over-annotation based on the gene name etymology rather than validated function.
GO:0046330 positive regulation of JNK cascade
IEA
GO_REF:0000117
ACCEPT
Summary: This is well-supported by experimental evidence. GADD45B activates MTK1/MEKK4 which in turn activates both p38 and JNK pathways [PMID:9827804]. However, GADD45B also inhibits JNK via MKK7 binding in certain contexts [PMID:25314077], making this context-dependent. The ARBA prediction is valid for the stress-responsive pathway.
Supporting Evidence:
PMID:9827804
Expression of the GADD45-like genes induces p38/JNK activation and apoptosis
GO:0051726 regulation of cell cycle
IEA
GO_REF:0000002
KEEP AS NON CORE
Summary: Consistent with IBA annotation. InterPro-based inference supports known GADD45 family function in cell cycle regulation via CRIF1 interaction [PMID:12716909].
Supporting Evidence:
PMID:12716909
CRIF1 binds specifically to the Gadd45 family proteins
GO:1900745 positive regulation of p38MAPK cascade
IEA
GO_REF:0000117
ACCEPT
Summary: This is strongly supported by experimental evidence. GADD45B activates MTK1/MEKK4 which activates MKK6, leading to p38 activation [PMID:9827804, PMID:12052864]. ARBA prediction is accurate.
Supporting Evidence:
PMID:12052864
GADD45 proteins bind a site in MTK1 near the inhibitory domain and relieve autoinhibition
GO:0005515 protein binding
IPI
PMID:12052864
Regulation of MTK1/MEKK4 kinase activity by its N-terminal a...
MODIFY
Summary: The vague term 'protein binding' should be replaced with a more specific MF term. This paper shows GADD45B binds MTK1/MEKK4 (a MAPKKK) and activates its kinase activity. MTK1/MEKK4 is a MAPKKK (MAP3K4).
Supporting Evidence:
PMID:12052864
By a functional complementation screening with yeast cells, GADD45 proteins (GADD45alpha, beta, and gamma) were identified as MTK1 activators. GADD45 proteins bind a site in MTK1 near the inhibitory domain and relieve autoinhibition
GO:0005515 protein binding
IPI
PMID:16256071
CIN85 regulates the ability of MEKK4 to activate the p38 MAP...
MODIFY
Summary: This paper shows CIN85 regulates MEKK4 activation by GADD45 proteins. The protein binding annotation is too vague - this involves the MTK1/MEKK4 activation pathway.
Supporting Evidence:
PMID:16256071
CIN85 was also shown to regulate the activation of MEKK4 by GADD45 proteins and promote multi-ubiquitination of MEKK4
GO:0005515 protein binding
IPI
PMID:25314077
Cancer-selective targeting of the NF-ΞΊB survival pathway wit...
MODIFY
Summary: This paper shows GADD45B binds directly to MKK7 and blocks its catalytic activity. MKK7 is a MAPKK (MAP2K7). Should be annotated to a more specific term.
Supporting Evidence:
PMID:25314077
GADD45Ξ² inhibits apoptosis by suppressing JNK signaling. It mediates this function by binding to the JNK kinase MKK7 and blocking its enzymatic activity by engaging the kinase catalytic pocket
GO:0005515 protein binding
IPI
PMID:32296183
A reference map of the human binary protein interactome.
REMOVE
Summary: This is a large-scale binary protein interactome study (HuRI). Generic 'protein binding' from high-throughput studies is not informative without mechanistic context.
Reason: High-throughput interactome study. Specific interactions should be curated from focused literature with mechanistic context rather than generic protein binding.
Supporting Evidence:
PMID:32296183
Here we present a human 'all-by-all' reference interactome map of human binary protein interactions, or 'HuRI'. With approximately 53,000 protein-protein interactions, HuRI has approximately four times as many such interactions as there are high-quality curated interactions from small-scale studies
GO:0005515 protein binding
IPI
PMID:33961781
Dual proteome-scale networks reveal cell-specific remodeling...
REMOVE
Summary: This is BioPlex 3.0, another large-scale protein interactome study. Same rationale as PMID:32296183 - generic protein binding from HT studies is not informative.
Reason: High-throughput interactome study. Specific interactions should be curated from focused literature with mechanistic context.
Supporting Evidence:
PMID:33961781
Through affinity-purification mass spectrometry, we have created two proteome-scale, cell-line-specific interaction networks. The first, BioPlex 3.0, results from affinity purification of 10,128 human proteins-half the proteome-in 293T cells and includes 118,162 interactions among 14,586 proteins
GO:0005634 nucleus
IDA
PMID:9827804
A family of stress-inducible GADD45-like proteins mediate ac...
ACCEPT
Summary: Direct experimental evidence for nuclear localization. This is a core localization for GADD45B's function in stress response signaling.
Supporting Evidence:
PMID:9827804
Using a yeast two-hybrid method, three related proteins, GADD45alpha (= GADD45), GADD45, (= MyD118), and GADD45gamma, were identified that bound to an N-terminal domain of MTK1
GO:0005737 cytoplasm
IDA
PMID:9827804
A family of stress-inducible GADD45-like proteins mediate ac...
ACCEPT
Summary: Direct experimental evidence for cytoplasmic localization. GADD45B is found in both nucleus and cytoplasm, consistent with its role in signaling between cellular compartments.
Supporting Evidence:
PMID:9827804
These proteins activated MTK1 kinase activity, both in vivo and in vitro
GO:0043065 positive regulation of apoptotic process
IDA
PMID:9827804
A family of stress-inducible GADD45-like proteins mediate ac...
ACCEPT
Summary: Well-supported by experimental evidence showing expression of GADD45-like genes induces p38/JNK activation and apoptosis. This reflects GADD45B's pro-apoptotic activity through MTK1/MEKK4 activation in response to stress.
Supporting Evidence:
PMID:9827804
Expression of the GADD45-like genes induces p38/JNK activation and apoptosis, which can be partially suppressed by coexpression of a dominant inhibitory MTK1 mutant protein
GO:0046330 positive regulation of JNK cascade
IDA
PMID:9827804
A family of stress-inducible GADD45-like proteins mediate ac...
ACCEPT
Summary: Well-supported by direct experimental evidence showing GADD45-like proteins mediate activation of the p38/JNK pathway via MTK1/MEKK4. This is a core function.
Supporting Evidence:
PMID:9827804
Expression of the GADD45-like genes induces p38/JNK activation and apoptosis
GO:1900745 positive regulation of p38MAPK cascade
IDA
PMID:9827804
A family of stress-inducible GADD45-like proteins mediate ac...
ACCEPT
Summary: Well-supported by direct experimental evidence [PMID:9827804]. Activation of MTK1/MEKK4 by GADD45B leads to p38 MAPK activation. This is a core function.
Supporting Evidence:
PMID:9827804
The stress-responsive p38 and JNK MAPK pathways regulate cell cycle and apoptosis. A human MAPKKK, MTK1 (= MEKK4), mediates activation of both p38 and JNK in response to environmental stresses
GO:0043066 negative regulation of apoptotic process
IDA
PMID:25314077
Cancer-selective targeting of the NF-ΞΊB survival pathway wit...
NEW
Summary: GADD45B suppresses JNK-mediated apoptosis by directly binding and inhibiting MKK7. This anti-apoptotic function is context-dependent, particularly relevant in NF-kB-driven cancer cells like multiple myeloma.
Supporting Evidence:
PMID:25314077
GADD45Ξ² suppresses JNK signaling and apoptosis by blocking MKK7 via direct physical interaction
file:human/GADD45B/GADD45B-deep-research-perplexity.md
GADD45B has also been identified as a promoter of cell survival through inhibition of JNK activation in multiple contexts

Core Functions

Binds to MTK1/MEKK4 (MAP3K4) N-terminal regulatory domain, relieving autoinhibition and activating downstream p38 and JNK MAPK pathways in response to environmental stress.

Supporting Evidence:
  • PMID:9827804
    These proteins activated MTK1 kinase activity, both in vivo and in vitro
  • PMID:12052864
    GADD45 proteins bind a site in MTK1 near the inhibitory domain and relieve autoinhibition.
  • file:human/GADD45B/GADD45B-deep-research-perplexity.md
    Upon stress stimulation, GADD45B binds to MTK1/MEKK4, enhancing the autophosphorylation and kinase activity of this upstream regulator, which subsequently leads to phosphorylation and activation of downstream p38 and JNK kinases

Binds directly to MKK7 (MAP2K7) and blocks its kinase activity, suppressing JNK-mediated apoptosis. This anti-apoptotic function is particularly relevant in cancer contexts where GADD45B acts downstream of NF-kB.

Supporting Evidence:
  • PMID:25314077
    The percentages of apoptotic cells are depicted.See also Figure S2.Development of D-Tetrapeptide Inhibitors of the GADD45Ξ²/MKK7 ComplexGiven the essential antiapoptotic role of GADD45Ξ² in MM and our previous results showing that GADD45Ξ² suppresses JNK signaling and apoptosis by blocking MKK7 via direct physical interaction (De Smaele et al., 2001, Papa et al., 2004, Papa et al., 2007), we aimed to develop selective inhibitors of this protein-protein interaction in order to induce cytotoxic JNK signaling in MM cells
  • file:human/GADD45B/GADD45B-deep-research-perplexity.md
    GADD45B directly binds to MKK7 and inhibits its catalytic activity toward JNK substrates, providing a mechanism through which GADD45B can attenuate JNK signaling in specific cellular contexts

References

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Suggested Questions for Experts

Q: How is the switch between GADD45B's pro-apoptotic function (MTK1/MEKK4 activation) and anti-apoptotic function (MKK7 inhibition) regulated in different cellular contexts?

Q: What is the structural basis for GADD45B's selective inhibition of MKK7 versus its activation of MTK1/MEKK4?

Suggested Experiments

Experiment: Solve the structure of GADD45B in complex with MTK1 and separately with MKK7 to understand the molecular basis for its opposing effects on these two kinases.

Type: protein structure

Experiment: Determine the relative binding affinities of GADD45B for MTK1 versus MKK7 and how these are modulated by NF-kB pathway activation.

Type: functional assay

Deep Research

Falcon

(GADD45B-deep-research-falcon.md)

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Perplexity

(GADD45B-deep-research-perplexity.md)

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