Affinage

EP300

Histone acetyltransferase p300 · UniProt Q09472

Length
2414 aa
Mass
264.2 kDa
Annotated
2026-06-09
100 papers in source corpus 36 papers cited in narrative 36 extracted findings
Cross-family judge vs UniProt: Affinage preferred faithfulness: 5/6 claims corpus-supported (83%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

EP300/p300 is a multifunctional lysine acyltransferase that writes activating chromatin marks and acts as a transcriptional adaptor bridging sequence-specific transcription factors to the basal machinery, where it was first identified as a TBP-associated component (PMID:8502484) and a direct p53-binding co-activator controlling cell-cycle checkpoint and apoptotic programs (PMID:9194565). Beyond histones (H3K27, H3K18, H2B), p300 acetylates a broad non-histone substrate set—MyoD (PMID:10944526), transition protein TP2 (PMID:19710011), the elongation factor AFF1 (PMID:31611376), NRF2 (PMID:32057361), NONO (PMID:34017080), FOXO3 (PMID:31357743), HSPA5 (PMID:37696842) and the mTORC1 component raptor (PMID:38267537)—coupling these modifications to muscle differentiation, chromatin condensation, transcriptional elongation, redox signaling, drug resistance and ferroptosis. Cryo-EM shows that p300 reads pre-existing H4 N-terminal acetylation through its bromodomain and directs catalysis to H2B tails to drive H2A-H2B eviction within the same nucleosome (PMID:37460559), and it potentiates transcription specifically on chromatinized templates (PMID:16109717). It also functions as a promiscuous acyltransferase, installing crotonylation (PMID:25818647, PMID:39080296), 2-hydroxyisobutyrylation (PMID:29775581) and succinylation (PMID:38256128) on histones and cytoplasmic glycolytic enzymes, linking acyl-CoA metabolism to gene expression and metabolic flux. p300 catalytic activity is held in check by intramolecular autoinhibition involving an autoinhibitory lysine-rich loop, the RING domain and the TAZ2 domain (PMID:30323286, PMID:37660055, PMID:36522330); this brake is relieved by transcription-factor-dimerization-driven trans-autoacetylation (PMID:30323286), by metabolite-derived acyl-CoAs that auto-acylate the loop (PMID:34677127), and by mTORC1 phosphorylation that prevents HAT-RING contact (PMID:29033323). Chromatin engagement is itself dictated by combinatorial transcription-factor inputs, with acetyltransferase activity opposing stable chromatin association (PMID:38159566). A spatially distinct cytoplasmic pool acts as an E3/E4 polyubiquitin ligase for p53 (PMID:19805293), and AMPK/PP2A-controlled phosphorylation at Ser89 governs nucleocytoplasmic shuttling that tunes raptor acetylation, mTORC1 activity and autophagy (PMID:38267537).

Mechanistic history

Synthesis pass · year-by-year structured walk · 29 steps
  1. 1993 Medium

    Established p300 as a physical component of the basal transcription apparatus, providing the first mechanistic anchor for its co-activator role.

    Evidence Co-immunoprecipitation with TBP and proteolytic peptide mapping

    PMID:8502484

    Open questions at the time
    • Did not define the functional consequence of the TBP interaction
    • Shared phosphoproteins (64/59 kDa) left unidentified
  2. 1997 High

    Showed p300 directly binds p53 and serves as a transcriptional adaptor controlling growth arrest and apoptosis, connecting it to tumor suppressor signaling.

    Evidence Reciprocal Co-IP, co-localization, and p21/bax promoter and cell-cycle/apoptosis assays

    PMID:9194565

    Open questions at the time
    • Did not resolve whether acetylation or scaffolding drives the effect
    • No structural basis for the interaction
  3. 2000 High

    Demonstrated that p300 acetylation of a non-histone substrate (MyoD) can directly activate that factor, broadening its enzymatic role beyond chromatin.

    Evidence In vitro acetylation, microinjection functional assay, acetylation-site mutagenesis

    PMID:10944526

    Open questions at the time
    • In vitro acetylation site relevance in vivo not fully mapped
    • Did not address chromatin context at the muscle promoter
  4. 2000 Medium

    Identified the first regulatory inputs onto p300—PKC phosphorylation at S89 (repressive) and the EID-1 HAT inhibitor—revealing that p300 activity is signal-controlled.

    Evidence In vivo phospho-site mapping plus kinase/reporter assays; yeast two-hybrid plus HAT inhibition assay

    PMID:11020388 PMID:11073990

    Open questions at the time
    • Structural mechanism of S89 phosphorylation effect not defined
    • EID-1 inhibition mechanism on the HAT domain unresolved
  5. 2005 High

    Established that p300 co-activation requires a nucleosomal template, linking its function mechanistically to histone hyperacetylation rather than naked-DNA transcription.

    Evidence Reconstituted in vitro transcription on chromatinized templates with Sox9 and ChIP

    PMID:16109717

    Open questions at the time
    • Specific histone residues responsible not pinned down here
    • Generalizability beyond the collagen enhancer untested
  6. 2009 High

    Revealed a compartment-specific moonlighting function: cytoplasmic p300/CBP act as an E4 polyubiquitin ligase that degrades p53, separating nuclear co-activation from cytoplasmic destruction.

    Evidence Subcellular fractionation, in vitro ubiquitination, domain mapping, p300/CBP-deficient cells

    PMID:19805293

    Open questions at the time
    • Catalytic mechanism of E4 activity within the N-terminal region not structurally defined
    • Regulation switching between HAT and ligase roles unclear
  7. 2009 High

    Extended the non-histone substrate repertoire and showed acetylation can disable a substrate's biophysical function, with TP2 acetylation reducing DNA condensation.

    Evidence In vitro acetylation, MS site mapping, CD and AFM, in vivo acetylation

    PMID:19710011

    Open questions at the time
    • Physiological role of TP2 acetylation during spermiogenesis not demonstrated in vivo
  8. 2009 High

    Provided a selective small-molecule (plumbagin) inhibitor and identified K1358 as critical for inhibitor binding, supporting the HAT domain as a druggable target.

    Evidence In vitro HAT assay, in vivo p53 acetylation, docking, site-directed mutagenesis

    PMID:19570987

    Open questions at the time
    • Selectivity over other acyltransferases in cells incomplete
    • Non-competitive mechanism not crystallographically resolved
  9. 2014 Medium

    Defined BAG6 as a controller of p300 nucleocytoplasmic distribution coupling p300 localization to autophagy regulation via differential substrate acetylation.

    Evidence Fractionation, Co-IP, knockout MEFs, acetylation and autophagy assays

    PMID:24852146

    Open questions at the time
    • Direct mechanism of BAG6-driven import not structurally defined
    • Relationship to later AMPK/S89 shuttling model not integrated here
  10. 2015 High

    Showed p300 is a crotonyltransferase whose activity is governed by cellular acyl-CoA levels, establishing it as a metabolic sensor that converts metabolite flux into transcriptional output.

    Evidence In vitro enzymatic assay, cell-based transcription, crotonyl-CoA perturbation, ChIP

    PMID:25818647

    Open questions at the time
    • Genomic distribution of crotonylation versus acetylation not fully mapped here
    • Selectivity determinants for acyl-CoA choice unresolved
  11. 2015 Medium

    Identified DDX24 as a negative regulator that blocks the p300-p53 interaction, adding to the network controlling p53 acetylation and senescence.

    Evidence Co-IP, RNAi, in vivo acetylation, p53 target expression

    PMID:25867071

    Open questions at the time
    • Direct versus indirect competition for p53 binding not distinguished
    • Single-lab finding without reciprocal structural data
  12. 2017 High

    Defined a direct mTORC1-to-p300 phosphorylation axis that relieves intramolecular HAT-RING autoinhibition, linking nutrient signaling to p300 activation, autophagy suppression and lipogenesis.

    Evidence Co-IP, in vitro kinase assay, domain-interaction mapping, autophagy/lipogenesis assays

    PMID:29033323

    Open questions at the time
    • Phospho-site to conformational change link inferred, not structurally captured
    • Crosstalk with other autoinhibitory domains not addressed
  13. 2018 High

    Captured the structural basis of p300 autoactivation: transcription-factor dimerization triggers trans-autoacetylation of an autoinhibitory loop that invades a neighboring active site.

    Evidence Crystal structure, in vitro HAT assay, mutagenesis, TF dimerization assays

    PMID:30323286

    Open questions at the time
    • In vivo kinetics of the trans-autoacetylation reaction not quantified
    • RING-domain rearrangement mechanism only partially defined
  14. 2018 High

    Discovered p300 as a 2-hydroxyisobutyryltransferase acting on glycolytic enzymes, directly coupling its enzymatic activity to metabolic flux and glucose-deprivation survival.

    Evidence In vitro assay, SILAC proteomics, MS, p300 KO cells, metabolic assays

    PMID:29775581

    Open questions at the time
    • Stoichiometry and reversibility of cytoplasmic Khib not defined
    • Site selectivity rules across substrates unresolved
  15. 2018 Medium

    Implicated DYRK1A as a kinase modulating p300/CBP enhancer activity, adding an enhancer-localized phospho-regulatory input to the network.

    Evidence MS interaction, Co-IP, ChIP-seq, shRNA with H3K27ac readout

    PMID:30137413

    Open questions at the time
    • Direct phosphorylation sites on p300 not mapped
    • Causality between phosphorylation and activity not biochemically isolated
  16. 2019 High

    Established a non-redundant, druggable role for EP300 (over CBP) in sustaining core regulatory enhancers, validated by selective PROTAC degradation causing enhancer collapse and apoptosis.

    Evidence CRISPR KO, JQAD1 PROTAC, ChIP-seq, Co-IP, xenograft

    PMID:34772733

    Open questions at the time
    • Molecular basis of EP300 vs CBP specificity at these enhancers unresolved
    • Generalizability beyond MYCN-amplified neuroblastoma untested here
  17. 2019 High

    Showed p300 acetylation of AFF1 dampens super-elongation-complex assembly and P-TEFb-dependent Pol II CTD phosphorylation, revealing a repressive role in transcriptional elongation under genotoxic stress.

    Evidence In vitro acetylation and P-TEFb kinase assays, mutagenesis rescue, ChIP

    PMID:31611376

    Open questions at the time
    • Genome-wide scope of stress-induced AFF1 acetylation not mapped
    • Interplay with p300's activating chromatin functions unresolved
  18. 2019 Medium

    Connected p300 acetylation to drug-response phenotypes, with FOXO3 acetylation promoting lapatinib sensitivity and NONO acetylation driving BRAF-inhibitor resistance via a p300-ERK feedback loop.

    Evidence Acetylation-deficient mutants, SIRT manipulation, ubiquitination assays, drug-sensitivity and in vivo resistance assays

    PMID:31357743 PMID:34017080

    Open questions at the time
    • Context-dependence of opposing drug-response outcomes not reconciled
    • Single-lab findings without independent replication
  19. 2020 Medium

    Showed p300 stabilizes NRF2 by disrupting NRF2-KEAP1 complex formation in a HAT-dependent manner, linking p300 to oxidative-stress transcriptional responses.

    Evidence Co-IP, knockdown/overexpression, fractionation, HAT-dead mutant

    PMID:32057361

    Open questions at the time
    • NRF2 acetylation site(s) not mapped
    • Direct versus indirect KEAP1 interference not resolved
  20. 2021 High

    Established that short-chain fatty acid-derived acyl-CoAs activate p300 by auto-acylating its autoinhibitory loop, mechanistically distinct from HDAC inhibition.

    Evidence Histone-modification proteomics, in vitro HAT assay, metabolite tracing, genetic/chemical perturbation

    PMID:34677127

    Open questions at the time
    • Relative contribution to histone acetylation versus HDAC inhibition in vivo not fully partitioned
  21. 2022 High

    Resolved how p300 reads and writes within a nucleosome: bromodomain recognition of H4 N-terminal acetylation directs catalysis to H2B tails, promoting H2A-H2B eviction.

    Evidence Cryo-EM structure, in vitro acetylation, nucleosome dissociation assay

    PMID:37460559

    Open questions at the time
    • Source of the initiating H4 acetylation not defined
    • Functional impact on transcription in cells not directly tested here
  22. 2022 High

    Defined the TAZ2 domain as a second autoinhibitory module whose conformational opening by transcription-factor binding (including oncogenic NUT) activates the HAT, unifying autoinhibition with feed-forward chromatin activation.

    Evidence HAT assays, domain truncation, ChIP-seq, NMR structure, cancer-mutation analysis

    PMID:36522330 PMID:37660055

    Open questions at the time
    • Quantitative interplay among RING, loop, and TAZ2 autoinhibition not integrated
    • How cancer mutations map onto each brake incompletely defined
  23. 2022 Medium

    Uncovered a non-enzymatic role for p300/CBP in sustaining Polycomb repression via Pol II pausing and R-loop formation, showing its function is not solely acetyltransferase-dependent.

    Evidence ChIP-seq, HAT-dead mutant, Drosophila and mouse cells, R-loop detection

    PMID:36206738

    Open questions at the time
    • Structural basis of HAT-independent Pol II stabilization unknown
    • Direct versus indirect contribution to PcG occupancy unresolved
  24. 2023 High

    Demonstrated that p300 chromatin association is dictated by combinatorial transcription-factor inputs and is opposed by its own catalytic activity, reframing how p300 is recruited genome-wide.

    Evidence Single-molecule tracking, systematic domain mutagenesis, U2OS cells

    PMID:38159566

    Open questions at the time
    • Identity of the dominant TF combinations at specific loci not enumerated
    • Mechanism by which acetylation reduces chromatin dwell-time unresolved
  25. 2023 Medium

    Defined deacetylase-mediated control of p300 output, with HDAC8 inactivating EP300 to redirect its TF-site occupancy and HDAC6/SIRT counter-regulating substrate acetylation in disease contexts.

    Evidence ATAC-seq, ChIP-seq, MS, HDAC inhibitor/loss-of-function, in vivo metastasis models

    PMID:37696842 PMID:38030596

    Open questions at the time
    • Autoacetylation sites removed by HDAC8 not fully mapped
    • Generalizability beyond melanoma/PDAC contexts untested
  26. 2023 High

    Established p300 as a writer of histone crotonylation (H3K18cr) essential for preimplantation embryo development, demonstrating developmental requirement for its acyltransferase function.

    Evidence Genetic depletion, RNA-seq, ChIP-seq, in vitro crotonylation assay

    PMID:39080296

    Open questions at the time
    • Relative developmental contribution of crotonylation versus acetylation not partitioned
  27. 2023 Medium

    Linked p300 acetylation to ferroptosis through HSPA5-K353 acetylation and YAP/ZEB-dependent LPCAT3 enhancer activation, connecting p300 to lipid-peroxidation cell-death control.

    Evidence Site mapping/mutagenesis, Co-IP, ChIP, luciferase reporter, ferroptosis assays, xenograft

    PMID:37166352 PMID:37696842

    Open questions at the time
    • Context-dependence of pro- versus anti-ferroptotic outcomes not reconciled
    • Single-lab findings per substrate
  28. 2024 High

    Integrated p300 localization into nutrient signaling: AMPK-dependent S89 phosphorylation drives nuclear entry that reduces raptor acetylation and mTORC1 activity to activate autophagy, with PP2A/CRM1 reversing the cycle, and progerin-driven mislocalization implicating the axis in Hutchinson-Gilford progeria.

    Evidence Fractionation, Co-IP, kinase/phosphatase and CRM1 manipulations, mouse tissue, patient cells

    PMID:38267537

    Open questions at the time
    • Structural basis of S89-dependent shuttling not defined
    • Reconciliation with earlier PKC-S89 repressive model not addressed
  29. 2024 Medium

    Showed p300 functions as a succinyltransferase on cytoplasmic glycolytic enzymes (PGK1), establishing succinylation as another metabolic-regulatory output of p300 in cancer.

    Evidence Succinylome proteomics, CRISPR KO, site mutagenesis, glycolysis/metabolomics

    PMID:38256128

    Open questions at the time
    • Cytoplasmic substrate selectivity rules undefined
    • Reversibility/desuccinylase counterpart not identified

Open questions

Synthesis pass · forward-looking unresolved questions
  • How the multiple autoinhibitory brakes (lysine-rich loop, RING, TAZ2), diverse acyl-CoA selectivity, compartment-specific catalytic versus ligase functions, and combinatorial TF-driven recruitment are coordinated into a single integrated regulatory logic remains unresolved.
  • No unified model linking acyl-CoA choice to substrate/site selection
  • Switch governing nuclear HAT versus cytoplasmic E4 ligase roles undefined
  • Quantitative hierarchy among the three autoinhibitory domains unknown

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0140096 catalytic activity, acting on a protein 8 GO:0016740 transferase activity 5 GO:0140110 transcription regulator activity 5 GO:0060090 molecular adaptor activity 3 GO:0042393 histone binding 2 GO:0016874 ligase activity 1
Localization
GO:0005829 cytosol 5 GO:0000228 nuclear chromosome 3 GO:0005634 nucleus 3
Pathway
R-HSA-4839726 Chromatin organization 5 R-HSA-74160 Gene expression (Transcription) 5 R-HSA-162582 Signal Transduction 4 R-HSA-5357801 Programmed Cell Death 3 R-HSA-9612973 Autophagy 3 R-HSA-1430728 Metabolism 2

Evidence

Reading pass · 36 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
1993 p300 co-precipitates with TATA-binding protein (TBP) in a specific, SDS-sensitive complex, and p300-specific and TBP-specific complexes share at least two common phosphoproteins (64 kDa and 59 kDa), indicating p300 interacts with TBP and is a component of the basal transcriptional machinery. Co-immunoprecipitation, partial proteolytic digest pattern matching Oncogene Medium 8502484
1997 p300 binds directly to the tumor suppressor p53 in the absence of viral oncoproteins; they colocalize in the nucleus and coexist in a stable DNA-binding complex. p300 acts as a transcriptional adaptor for p53, modulating its G1 checkpoint and apoptosis functions. E1A disrupts p300/p53-dependent growth control. Co-immunoprecipitation, co-localization, functional promoter assays (p21, bax), cell-cycle and apoptosis assays Nature High 9194565
2000 p300 and CBP acetylate MyoD on two lysines at the boundary of the DNA-binding domain in vitro; this acetylation activates MyoD transcriptional activity on a muscle-specific promoter. MyoD mutants that cannot be acetylated are not functionally activated. In vitro acetylation assay, microinjection functional assay, mutagenesis The Journal of biological chemistry High 10944526
2000 Protein kinase C phosphorylates p300 at serine 89 in vivo; this phosphorylation represses the transcriptional activity of p300, representing a signal transduction pathway for PKC to regulate cell growth and differentiation. In vivo phosphorylation mapping, kinase assay, transcriptional reporter assay The Journal of biological chemistry Medium 11020388
2000 EID-1 binds p300 and inhibits its histone acetyltransferase activity, thereby repressing MyoD-dependent transcription in skeletal muscle independently of its Rb-binding function. Yeast two-hybrid, co-immunoprecipitation, HAT activity assay, transcriptional reporter assay Molecular and cellular biology Medium 11073990
2003 p29ING4 and p28ING5 physically interact with p300 in vivo and enhance p300-mediated acetylation of p53 at Lys-382, thereby activating p53-dependent transcription and apoptosis. Co-immunoprecipitation, in vivo acetylation assay, transcriptional reporter assay (p21/waf1 promoter) Cancer research Medium 12750254
2003 p68 RNA helicase directly interacts with multiple domains of CBP/p300 and with RNA Pol II in vivo and in vitro; p68 stimulates CBP/p300-mediated transcription in a cooperative manner, and E1A suppression of CBP/p300 abolishes p68-driven transcription. Co-immunoprecipitation, GST pulldown, transcriptional reporter assay Oncogene Medium 12527917
2005 p300 potentiates Sox9-dependent transcription specifically on chromatinized (nucleosomal) DNA templates but not on naked DNA, and this is associated with p300-mediated histone hyperacetylation around the collagen α1(II) enhancer. In vitro transcription on chromatinized templates, recombinant protein association assay, ChIP The Journal of biological chemistry High 16109717
2006 Nuclear ROCK2 associates with and phosphorylates p300 both in vitro and in cells; ROCK2-mediated phosphorylation of p300 increases its acetyltransferase activity in vitro. Co-immunoprecipitation, in vitro kinase assay, gel filtration, immunofluorescence co-localization, HAT activity assay The Journal of biological chemistry Medium 16574662
2009 p300 and CBP function as cytoplasmic E4 polyubiquitin ligases for p53. The E3/E4 ubiquitin ligase activity resides exclusively in cytoplasmic fractions; the N-terminal ~595 aa of p300 encode both E3 and p53-directed E4 activities. CBP deficiency specifically stabilizes cytoplasmic, but not nuclear, p53. Subcellular fractionation, in vitro ubiquitination assay, co-immunoprecipitation, loss-of-function cell lines (p300/CBP-deficient) Proceedings of the National Academy of Sciences of the United States of America High 19805293
2009 KAT3B/p300 acetylates transition protein 2 (TP2) more efficiently than PCAF in vitro, targeting four lysine residues in the C-terminal domain. Acetylation of TP2 by p300 reduces its DNA condensation ability and impedes its interaction with the histone chaperone NPM3. In vitro acetyltransferase assay, mass spectrometry, circular dichroism, atomic force microscopy, in vivo acetylation The Journal of biological chemistry High 19710011
2009 The natural hydroxynaphthoquinone plumbagin inhibits p300 HAT activity in a non-competitive manner in vitro and in vivo, specifically blocking p300-mediated (but not PCAF-mediated) acetylation of p53. Site-directed mutagenesis of K1358 in the HAT domain abolishes inhibitor binding. In vitro HAT assay, in vivo p53 acetylation assay, molecular docking, site-directed mutagenesis The Journal of biological chemistry High 19570987
2014 BAG6 regulates nuclear localization of EP300; in the absence of BAG6, EP300 accumulates in the cytoplasm. BAG6 interaction with EP300 occurs in the cytoplasm and during starvation promotes EP300 translocation to the nucleus, where it acetylates p53 (pro-autophagic) while reducing cytoplasmic acetylation of ATG5, ATG7, and LC3-I (which inhibit autophagy). Subcellular fractionation, co-immunoprecipitation, loss-of-function (knockout MEFs), acetylation assays, autophagy assays Autophagy Medium 24852146
2015 p300 has both acetyltransferase and crotonyltransferase activities; p300-catalyzed histone crotonylation directly stimulates transcription to a greater degree than histone acetylation. Cellular crotonyl-CoA concentration regulates histone crotonylation levels and thereby gene expression. In vitro enzymatic assay, cell-based transcription assay, genetic/environmental perturbation of crotonyl-CoA levels, ChIP Molecular cell High 25818647
2015 DDX24 interacts with p300 and suppresses p300-mediated acetylation of p53. DDX24 overexpression inhibits the p300-p53 interaction; knockdown of DDX24 increases p53 acetylation levels, activates p53 target genes (p21, PUMA), and induces cell cycle arrest and senescence in a p53-dependent manner. Co-immunoprecipitation, RNA interference, in vivo acetylation assay, transcriptional target expression Oncogene Medium 25867071
2017 mTORC1 directly interacts with p300 and phosphorylates it at four serine residues in the C-terminal domain. This phosphorylation prevents the HAT domain from binding the RING domain, relieving intramolecular autoinhibition of p300. mTORC1-dependent p300 phosphorylation suppresses starvation-induced autophagy and activates lipogenesis. Co-immunoprecipitation, in vitro kinase assay, domain interaction mapping, functional autophagy and lipogenesis assays Molecular cell High 29033323
2018 p300 functions as a lysine 2-hydroxyisobutyryltransferase (Khib writer), targeting distinct sites from its acetylation targets. p300-catalyzed Khib on glycolytic enzymes (e.g., ENO1) regulates their catalytic activity; p300 deletion reduces Khib on these enzymes, impairs glycolysis, and sensitizes cells to glucose deprivation-induced death. In vitro enzymatic assay, quantitative proteomics (SILAC), mass spectrometry, genetic deletion (p300 KO cells), metabolic activity assay Molecular cell High 29775581
2018 Transcription factor dimerization (IRF3, STAT1) activates p300 by enabling trans-autoacetylation of p300's autoinhibitory lysine-rich loop. A crystal structure of p300 shows the autoinhibitory loop invading the active site of a neighboring HAT domain, capturing a trans-autoacetylation intermediate. The RING domain also has an autoinhibitory role requiring rearrangement for substrate access. Crystal structure, in vitro HAT assay, mutagenesis, transcription factor dimerization assays Nature High 30323286
2018 DYRK1A physically interacts with p300 and CBP; overexpression of DYRK1A causes hyperphosphorylation of p300/CBP. ChIP-seq shows DYRK1A co-localizes with p300/CBP at enhancers; DYRK1A knockdown reduces H3K27ac at these enhancers, indicating DYRK1A modulates p300/CBP acetyltransferase activity at enhancers. Proteomics (mass spectrometry), co-immunoprecipitation, ChIP-seq, shRNA knockdown with H3K27ac readout Nucleic acids research Medium 30137413
2019 EP300 controls enhancer acetylation by interacting with TFAP2β, a lineage-defining transcription factor in MYCN-amplified neuroblastoma. EP300 (but not CBP) is essential for H3K27ac at core regulatory circuitry enhancers; PROTAC-mediated degradation of EP300 (JQAD1) causes loss of H3K27ac at these enhancers and rapid apoptosis in a CRBN-dependent manner. CRISPR KO, PROTAC degrader, ChIP-seq, co-immunoprecipitation, in vivo xenograft Cancer discovery High 34772733
2019 AFF1 (a super elongation complex subunit) is site-specifically acetylated by p300; this acetylation reduces AFF1 interaction with other SEC components and impairs P-TEFb-mediated RNA Pol II CTD phosphorylation both in vitro and in vivo. Upon genotoxic stress, p300-mediated AFF1 acetylation correlates with global transcriptional downregulation, and acetylation-defective AFF1 rescues transcription. In vitro acetylation and P-TEFb kinase assays, co-immunoprecipitation, mutagenesis, ChIP, genotoxic stress experiments Proceedings of the National Academy of Sciences of the United States of America High 31611376
2020 p300 physically interacts with NRF2 and interferes with NRF2-KEAP1 complex formation, thereby increasing NRF2 protein stability and promoting its nuclear localization. The acetyltransferase activity of p300 is indispensable for these stabilizing effects. Co-immunoprecipitation, overexpression/knockdown, nuclear fractionation, HAT-dead mutant analysis, cell viability assay Biochemical and biophysical research communications Medium 32057361
2021 Short-chain fatty acids propionate and butyrate (but not acetate) activate p300 acetyltransferase by being converted to acyl-CoAs that are used by p300 to catalyze auto-acylation of the autoinhibitory loop, resulting in enzyme activation and global histone acetylation—distinct from HDAC inhibition. Quantitative proteomics of histone modifications, in vitro HAT assay, metabolite tracing, genetic/chemical perturbation eLife High 34677127
2022 Cryo-EM structures reveal that p300/CBP recognizes histone H4 N-terminal tail acetylation via its bromodomain (and contacts DNA minor grooves outside the pocket), directing the catalytic center to non-H4 histone tails within the same nucleosome. The primary write target after reading H4NTac is H2BNT; H2BNTac promotes H2A-H2B dissociation from the nucleosome. Cryo-EM structure, in vitro acetyltransferase assay, nucleosome dissociation assay Nature communications High 37460559
2022 The TAZ2 domain of p300 has an autoinhibitory function for HAT activity. Truncation of TAZ2 leads to hyperactive HAT and elevated H3K27ac and H3K18ac. Mechanistically, TAZ2 cooperates with neighboring HAT domains to maintain the active site in a 'closed' state; binding of transcription factors to TAZ2 or TAZ2 truncation induces a conformational opening of the active site. HAT activity assay, domain truncation mutagenesis, ChIP-seq, structural modeling, cancer mutation analysis Nature communications High 37660055
2022 NUT (in the BRD4-NUT oncoprotein) contains an acidic transcriptional activation domain that binds the TAZ2 domain of p300, allosterically activating p300. NUT-TAZ2 interaction or cancer mutations interfering with TAZ2 autoinhibition activate p300, leading to a self-organizing, acetylation-dependent feed-forward reaction enabling long-range chromatin interactions via bromodomain multivalent acetyl-lysine binding. NMR structure, in vitro acetyltransferase assay, mutagenesis, co-immunoprecipitation Nature communications High 36522330
2023 EP300 acetylates HSPA5 (GRP78) at K353, and this acetylation reduces HSPA5's ability to inhibit lipid peroxidation, thereby promoting ferroptosis. HDAC6 limits HSPA5 acetylation and subsequent ferroptosis. Genetic or pharmacological inhibition of EP300 increases PDAC cell resistance to ferroptosis. Acetylation site mapping, mutagenesis (K353 site), genetic and pharmacological inhibition, ferroptosis assays, co-immunoprecipitation Scientific reports Medium 37696842
2023 p300 functions as a writer of histone crotonylation during preimplantation embryo development. P300 depletion causes developmental defects and transcriptome dysregulation. H3K18 crotonylation (H3K18cr), catalyzed by P300, localizes to active promoter regions and activates gene transcription required for embryo development. Genetic depletion (microinjection), RNA-seq, ChIP-seq, in vitro crotonylation assay Nature communications High 39080296
2023 p300 is an obligate integrator of combinatorial transcription factor inputs for chromatin binding: systematic mutagenesis of all annotated p300 domains in live cells shows that chromatin association depends entirely on combinatorial binding through multiple TF-interaction domains. p300 acetyltransferase activity opposes its chromatin association, and N-terminal TF-interaction domains regulate catalytic activity. Single-molecule tracking (live cell imaging), domain mutagenesis, U2OS cells Molecular cell High 38159566
2023 HDAC8 deacetylates EP300, causing its enzymatic inactivation. This inactivation increases EP300 binding to Jun-transcriptional sites and decreases binding to MITF-transcriptional sites, altering chromatin accessibility and driving a neural crest-stem cell transcriptional state promoting melanoma brain metastasis. ATAC-seq, ChIP-seq, HDAC8 inhibitor treatment, loss-of-function, mass spectrometry Nature communications Medium 38030596
2023 EP300 acetylates raptor (mTORC1 component), and nucleus-cytoplasmic shuttling of p300/EP300 regulates mTORC1 activity in response to amino acid or glucose levels. Nutrient deprivation causes AMPK-dependent phosphorylation of p300 at serine 89, promoting its cytoplasm-to-nucleus relocalization, reducing raptor acetylation and mTORC1 activity, and activating autophagy. Nutrient repletion causes PP2A-dependent dephosphorylation of nuclear p300, enabling CRM1-dependent nuclear export and mTORC1 reactivation. In Hutchinson-Gilford progeria syndrome, progerin mislocalizes p300 to the cytoplasm, hyperactivating mTORC1. Subcellular fractionation, co-immunoprecipitation, siRNA knockdown, AMPK inhibition, CRM1 inhibition, in vivo mouse tissue analysis, patient cell lines Nature cell biology High 38267537
2024 p300 functions as a succinylation writer (succinyl-CoA transferase) for cytoplasmic proteins including glycolytic enzymes. EP300 deletion leads to systemic reduction of lysine succinylation; p300-mediated succinylation of PGK1 promotes glycolysis, and mutation of the succinylated site of PGK1 impairs glycolysis and lactate production in lung cancer cells. Succinylome proteomics (SILAC/MS), CRISPR KO of EP300, site mutagenesis, glycolysis/metabolomics assays International journal of molecular sciences Medium 38256128
2019 EP300 acetylates FOXO3, and this acetylation promotes lapatinib sensitivity in HER2-positive breast cancer cells. Ectopic expression of wild-type but not acetylation-deficient EP300 increases acetylated-FOXO3 and lapatinib cytotoxicity; SIRT1/6 deacetylate FOXO3, counteracting EP300 activity. Ectopic expression, acetylation-deficient mutant, SIRT1/6 siRNA/inhibitor, drug sensitivity assay, ChIP Cancers Medium 31357743
2019 p300 catalyzes acetylation of NONO at K198, stabilizing NONO by antagonizing its RNF8-mediated ubiquitination/degradation. NONO stabilizes CRAF and ARAF, reactivating pERK1/2 and promoting BRAF inhibitor resistance in melanoma. ERK1/2 activation feeds back to induce p300, forming a positive feedback loop. Co-immunoprecipitation, in vitro acetylation assay, mutagenesis, ubiquitination assay, in vitro/in vivo drug resistance assays Oncogene Medium 34017080
2022 p300/CBP sustains Polycomb-group protein occupancy at repressive sites by non-enzymatic functions: CBP stabilizes RNA Pol II at PcG-bound sites and promotes Pol II pausing independently of HAT activity. CBP/Pol II pausing is required for R-loop formation and nucleosome depletion at Polycomb Response Elements. ChIP-seq, genetic manipulation in Drosophila and mouse cells, HAT-dead mutant, R-loop detection Molecular cell Medium 36206738
2023 EP300 interacts with YAP and ZEB (via its Bromo domain and CBP/p300-HAT domain respectively) and simultaneously binds these factors to induce H3K27 acetylation at the LPCAT3 promoter, activating LPCAT3 transcription and thereby promoting ferroptosis sensitivity in lung adenocarcinoma cells. Co-immunoprecipitation, ChIP-qPCR, dual-luciferase reporter, xenograft model, domain interaction mapping Antioxidants & redox signaling Medium 37166352

Source papers

Stage 0 corpus · 100 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2001 p300/CBP proteins: HATs for transcriptional bridges and scaffolds. Journal of cell science 898 11559745
1997 Binding and modulation of p53 by p300/CBP coactivators. Nature 620 9194565
2004 p300/CBP and cancer. Oncogene 521 15156177
2015 Intracellular crotonyl-CoA stimulates transcription through p300-catalyzed histone crotonylation. Molecular cell 500 25818647
2004 CBP and p300: HATs for different occasions. Biochemical pharmacology 383 15313412
1998 Conjunction dysfunction: CBP/p300 in human disease. Trends in genetics : TIG 343 9613201
2003 p29ING4 and p28ING5 bind to p53 and p300, and enhance p53 activity. Cancer research 240 12750254
1999 p300 and CBP: partners for life and death. Journal of cellular physiology 240 10497301
2021 Targeting the p300/CBP Axis in Lethal Prostate Cancer. Cancer discovery 237 33431496
2022 Histone acetyltransferases CBP/p300 in tumorigenesis and CBP/p300 inhibitors as promising novel anticancer agents. Theranostics 202 35836809
2017 Exploitation of EP300 and CREBBP Lysine Acetyltransferases by Cancer. Cold Spring Harbor perspectives in medicine 175 27881443
2011 Quercetin suppresses cyclooxygenase-2 expression and angiogenesis through inactivation of P300 signaling. PloS one 171 21857970
2018 p300-Mediated Lysine 2-Hydroxyisobutyrylation Regulates Glycolysis. Molecular cell 157 29775581
2007 The transcriptional coactivator and acetyltransferase p300 in fibroblast biology and fibrosis. Journal of cellular physiology 155 17559085
2018 Transcription factor dimerization activates the p300 acetyltransferase. Nature 147 30323286
2017 mTORC1 Phosphorylates Acetyltransferase p300 to Regulate Autophagy and Lipogenesis. Molecular cell 143 29033323
2022 EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma. Cancer discovery 140 34772733
2021 Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell chemical biology 136 33400925
2005 Sox9 and p300 cooperatively regulate chromatin-mediated transcription. The Journal of biological chemistry 129 16109717
1993 p300, and p300-associated proteins, are components of TATA-binding protein (TBP) complexes. Oncogene 126 8502484
2009 CBP and p300 are cytoplasmic E4 polyubiquitin ligases for p53. Proceedings of the National Academy of Sciences of the United States of America 124 19805293
2007 Expression of HDAC1 and CBP/p300 in human colorectal carcinomas. Journal of clinical pathology 124 17720775
2021 Short-chain fatty acids activate acetyltransferase p300. eLife 116 34677127
2019 Brd4 and P300 Confer Transcriptional Competency during Zygotic Genome Activation. Developmental cell 109 31211993
2000 CREB-binding protein/p300 activates MyoD by acetylation. The Journal of biological chemistry 107 10944526
2000 A novel Rb- and p300-binding protein inhibits transactivation by MyoD. Molecular and cellular biology 105 11073990
2009 Inhibition of lysine acetyltransferase KAT3B/p300 activity by a naturally occurring hydroxynaphthoquinone, plumbagin. The Journal of biological chemistry 102 19570987
2000 Phosphorylation of p300 at serine 89 by protein kinase C. The Journal of biological chemistry 102 11020388
1996 p300 and CBP as transcriptional regulators and targets of oncogenic events. Biological chemistry 101 8960368
2003 Synergism between p68 RNA helicase and the transcriptional coactivators CBP and p300. Oncogene 98 12527917
2023 LPCAT3 Is Transcriptionally Regulated by YAP/ZEB/EP300 and Collaborates with ACSL4 and YAP to Determine Ferroptosis Sensitivity. Antioxidants & redox signaling 97 37166352
2023 Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies. Cancer cell 92 37995682
2006 Nuclear Rho kinase, ROCK2, targets p300 acetyltransferase. The Journal of biological chemistry 88 16574662
2023 METTL14 regulates microglia/macrophage polarization and NLRP3 inflammasome activation after ischemic stroke by the KAT3B-STING axis. Neurobiology of disease 83 37541353
2019 Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming. Nature chemical biology 77 30962627
2023 The Role of CREBBP/EP300 and Its Therapeutic Implications in Hematological Malignancies. Cancers 71 36831561
2016 Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition. The Journal of biological chemistry 71 27056325
2016 CBP/p300 acetyltransferase activity in hematologic malignancies. Molecular genetics and metabolism 70 27380996
2017 Activation and overexpression of Sirt1 attenuates lung fibrosis via P300. Biochemical and biophysical research communications 66 28365154
2020 EP300 mutation is associated with tumor mutation burden and promotes antitumor immunity in bladder cancer patients. Aging 64 32012118
2002 Mutation analysis of EP300 in colon, breast and ovarian carcinomas. International journal of cancer 63 12385008
2020 Antitumor activity of the dual BET and CBP/EP300 inhibitor NEO2734. Blood advances 61 32882003
2023 Epigenetic mechanisms to propagate histone acetylation by p300/CBP. Nature communications 60 37460559
2020 Differential contribution of p300 and CBP to regulatory element acetylation in mESCs. BMC molecular and cell biology 58 32690000
2023 Lactate-induced histone lactylation by p300 promotes osteoblast differentiation. PloS one 56 38051708
2016 P300 inhibition enhances gemcitabine-induced apoptosis of pancreatic cancer. Oncotarget 56 27322077
2022 Structural insights into p300 regulation and acetylation-dependent genome organisation. Nature communications 55 36522330
2018 Modulating the masters: chemical tools to dissect CBP and p300 function. Current opinion in chemical biology 55 30025258
2020 The acetyltransferase p300 regulates NRF2 stability and localization. Biochemical and biophysical research communications 51 32057361
2020 p300 in Cardiac Development and Accelerated Cardiac Aging. Aging and disease 50 32765954
2019 MITF Expression Predicts Therapeutic Vulnerability to p300 Inhibition in Human Melanoma. Cancer research 49 30910803
2023 p300 is an obligate integrator of combinatorial transcription factor inputs. Molecular cell 46 38159566
2004 Expression of p300 protects cardiac myocytes from apoptosis in vivo. Biochemical and biophysical research communications 44 14975762
2015 Negative regulation of the p300-p53 interplay by DDX24. Oncogene 43 25867071
2015 High-density P300 enhancers control cell state transitions. BMC genomics 41 26546038
2018 Inhibition of EP300 and DDR1 synergistically alleviates pulmonary fibrosis in vitro and in vivo. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 40 30119248
2002 Acetyltransferase machinery conserved in p300/CBP-family proteins. Oncogene 38 11948408
2000 Viral replication and the coactivators p300 and CBP. Trends in microbiology 38 11115752
2023 EGR1 induces EMT in pancreatic cancer via a P300/SNAI2 pathway. Journal of translational medicine 37 36932397
2014 BAG6/BAT3 modulates autophagy by affecting EP300/p300 intracellular localization. Autophagy 37 24852146
2019 EP300 and SIRT1/6 Co-Regulate Lapatinib Sensitivity Via Modulating FOXO3-Acetylation and Activity in Breast Cancer. Cancers 35 31357743
2016 Loss of p300 accelerates MDS-associated leukemogenesis. Leukemia 34 27881875
2018 DYRK1A interacts with histone acetyl transferase p300 and CBP and localizes to enhancers. Nucleic acids research 32 30137413
2023 Cardiac Aging Is Promoted by Pseudohypoxia Increasing p300-Induced Glycolysis. Circulation research 31 37681309
2015 The LIM protein Ajuba promotes adipogenesis by enhancing PPARγ and p300/CBP interaction. Cell death and differentiation 31 26113042
2024 p300 nucleocytoplasmic shuttling underlies mTORC1 hyperactivation in Hutchinson-Gilford progeria syndrome. Nature cell biology 29 38267537
2023 EP300 as a Molecular Integrator of Fibrotic Transcriptional Programs. International journal of molecular sciences 29 37569677
2023 EP300 promotes ferroptosis via HSPA5 acetylation in pancreatic cancer. Scientific reports 29 37696842
1999 The coactivators p300 and CBP have different functions during the differentiation of F9 cells. Journal of molecular medicine (Berlin, Germany) 29 10475063
2023 HDAC8-mediated inhibition of EP300 drives a transcriptional state that increases melanoma brain metastasis. Nature communications 28 38030596
2022 p300/CBP sustains Polycomb silencing by non-enzymatic functions. Molecular cell 28 36206738
2017 Downregulation of decidual SP1 and P300 is associated with severe preeclampsia. Journal of molecular endocrinology 28 29273682
2023 EP300 facilitates human trophoblast stem cell differentiation. Proceedings of the National Academy of Sciences of the United States of America 27 37406095
2016 CBP/p300 acetyltransferases regulate the expression of NKG2D ligands on tumor cells. Oncogene 27 27477692
2014 Naphthoquinone-mediated inhibition of lysine acetyltransferase KAT3B/p300, basis for non-toxic inhibitor synthesis. The Journal of biological chemistry 27 24469461
2005 GCN5 and p300 share essential functions during early embryogenesis. Developmental dynamics : an official publication of the American Association of Anatomists 26 15937931
2020 p300 is upregulated by docetaxel and is a target in chemoresistant prostate cancer. Endocrine-related cancer 25 31951590
2018 Epstein-Barr Virus Nuclear Antigen Leader Protein Coactivates EP300. Journal of virology 24 29467311
2009 Interleukin-4 activates androgen receptor through CBP/p300. The Prostate 24 18819102
2024 Genetic dysregulation of EP300 in cancers in light of cancer epigenome control - targeting of p300-proficient and -deficient cancers. Molecular therapy. Oncology 23 39351073
2018 Enhancer RNA and NFκB-dependent P300 regulation of ADAMDEC1. Molecular immunology 23 30352365
2022 Analysis and therapeutic targeting of the EP300 and CREBBP acetyltransferases in anaplastic large cell lymphoma and Hodgkin lymphoma. Leukemia 22 36456744
2024 P300 regulates histone crotonylation and preimplantation embryo development. Nature communications 21 39080296
2023 PPARα Senses Bisphenol S to Trigger EP300-Mediated Autophagy Blockage and Hepatic Steatosis. Environmental science & technology 21 38085933
2018 Chemical and genetic rescue of an ep300 knockdown model for Rubinstein Taybi Syndrome in zebrafish. Biochimica et biophysica acta. Molecular basis of disease 21 29409755
2022 The acetyltransferase p300 is recruited in trans to multiple enhancer sites by lncSmad7. Nucleic acids research 20 35137201
2020 DBC1, p300, HDAC3, and Siah1 coordinately regulate ELL stability and function for expression of its target genes. Proceedings of the National Academy of Sciences of the United States of America 20 32152128
2024 Acetyltransferase P300 Regulates Glucose Metabolic Reprogramming through Catalyzing Succinylation in Lung Cancer. International journal of molecular sciences 19 38256128
2022 TWIST1-EP300 Expedites Gastric Cancer Cell Resistance to Apatinib by Activating the Expression of COL1A2. Analytical cellular pathology (Amsterdam) 19 35242497
2021 Targeting the p300/NONO axis sensitizes melanoma cells to BRAF inhibitors. Oncogene 19 34017080
2020 A Novel E2F1-EP300-VMP1 Pathway Mediates Gemcitabine-Induced Autophagy in Pancreatic Cancer Cells Carrying Oncogenic KRAS. Frontiers in endocrinology 19 32655498
2016 Histone acetyltransferease p300 modulates TIM4 expression in dendritic cells. Scientific reports 19 26899911
2019 AFF1 acetylation by p300 temporally inhibits transcription during genotoxic stress response. Proceedings of the National Academy of Sciences of the United States of America 18 31611376
2019 Coordinated expression of p300 and HDAC3 upregulates histone acetylation during dentinogenesis. Journal of cellular biochemistry 18 31692090
2023 A novel lncRNA SNHG29 regulates EP300- related histone acetylation modification and inhibits FLT3-ITD AML development. Leukemia 17 37157016
2023 TAZ2 truncation confers overactivation of p300 and cellular vulnerability to HDAC inhibition. Nature communications 17 37660055
2022 Role of p300, a histone acetyltransferase enzyme, in osteoblast differentiation. Differentiation; research in biological diversity 17 35180610
2017 ING5 differentially regulates protein lysine acetylation and promotes p300 autoacetylation. Oncotarget 17 29416718
2009 Acetylation of transition protein 2 (TP2) by KAT3B (p300) alters its DNA condensation property and interaction with putative histone chaperone NPM3. The Journal of biological chemistry 17 19710011
2024 HDAC6 inhibition disrupts HDAC6-P300 interaction reshaping the cancer chromatin landscape. Clinical epigenetics 15 39155390

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