E1A binding protein p300

Target id: 2735

Nomenclature: E1A binding protein p300

Family: Non-enzymatic BRD containing proteins

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     E1A binding protein p300 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2414 22q13.2 EP300 E1A binding protein p300
Mouse - 2412 15 E1 Ep300 E1A binding protein p300
Rat - - 7q34 Ep300 E1A binding protein p300
Previous and Unofficial Names
histone acetyltransferase p300 | KAT3B
Database Links
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the bromodomain of human EP300
PDB Id:  3I3J
Resolution:  2.33Å
Species:  Human
References:  6

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
I-CBP112 Hs Inhibition 6.2 pKd 10
pKd 6.2 (Kd 6.25x10-7 M) [10]
Description: Isothermal titration calorimetry (ITC) assay.
C646 Hs Inhibition 6.4 pKi 4
pKi 6.4 (Ki 4x10-7 M) [4]
SGC-CBP30 Hs Inhibition 7.4 pIC50 7
pIC50 7.4 (IC50 3.8x10-8 M) [7]
Lys-CoA Hs Inhibition 6.3 pIC50 8
pIC50 6.3 (IC50 5x10-7 M) [8]
anacardic acid Hs Inhibition 5.3 pIC50 2
pIC50 5.3 (IC50 5x10-6 M) [2]
garcinol Hs Inhibition 5.2 pIC50 1
pIC50 5.2 (IC50 7x10-6 M) [1]
curcumin Hs Inhibition 4.6 pIC50 3
pIC50 4.6 (IC50 2.5x10-5 M) [3]
plumbagin Hs Inhibition 4.6 pIC50 9
pIC50 4.6 (IC50 2.5x10-5 M) [9]
epigallocatechin-3-gallate Hs Inhibition 4.5 pIC50 5
pIC50 4.5 (IC50 3x10-5 M) [5]
H3-CoA-20 Hs Inhibition 3.7 pIC50 8
pIC50 3.7 (IC50 2x10-4 M) [8]
Immunopharmacology Comments
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. PMID: 26261308
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process ID:  2
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  stimulatory C-type lectin receptor signaling pathway (GO:0002223) TAS
References: 
Immuno Process:  Immune regulation
Immuno Process ID:  6
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  stimulatory C-type lectin receptor signaling pathway (GO:0002223) TAS
regulation of megakaryocyte differentiation (GO:0045652) TAS
References: 
Immuno Process:  Cytokine production & signalling
Immuno Process ID:  9
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  positive regulation of type I interferon production (GO:0032481) TAS
References: 
Immuno Process:  Cellular signalling
Immuno Process ID:  11
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  stimulatory C-type lectin receptor signaling pathway (GO:0002223) TAS
B cell differentiation (GO:0030183) IEA
References: 
Immuno Process:  B cell (activation)
Immuno Process ID:  5
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  B cell differentiation (GO:0030183) IEA
References: 
Immuno Process:  Immune system development
Immuno Process ID:  8
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  B cell differentiation (GO:0030183) IEA
platelet formation (GO:0030220) IEA
megakaryocyte development (GO:0035855) IEA
regulation of megakaryocyte differentiation (GO:0045652) TAS
References: 
Clinically-Relevant Mutations and Pathophysiology
Disease:  Colorectal cancer
Disease Ontology: DOID:9256
OMIM: 114500
Disease:  Rubinstein-Taybi syndrome 2; RSTS2
Synonyms: Rubinstein-Taybi syndrome [Disease Ontology: DOID:1933]
Rubinstein-Taybi syndrome due to EP300 haploinsufficiency [Orphanet: ORPHA353284]
Disease Ontology: DOID:1933
OMIM: 613684
Orphanet: ORPHA353284

References

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1. Balasubramanyam K, Altaf M, Varier RA, Swaminathan V, Ravindran A, Sadhale PP, Kundu TK. (2004) Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression. J. Biol. Chem.279 (32): 33716-26. [PMID:15155757]

2. Balasubramanyam K, Swaminathan V, Ranganathan A, Kundu TK. (2003) Small molecule modulators of histone acetyltransferase p300. J. Biol. Chem.278 (21): 19134-40. [PMID:12624111]

3. Balasubramanyam K, Varier RA, Altaf M, Swaminathan V, Siddappa NB, Ranga U, Kundu TK. (2004) Curcumin, a novel p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. J. Biol. Chem.279 (49): 51163-71. [PMID:15383533]

4. Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA, Liszczak G, Yuan H et al.. (2010) Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem. Biol.17 (5): 471-82. [PMID:20534345]

5. Choi KC, Jung MG, Lee YH, Yoon JC, Kwon SH, Kang HB, Kim MJ, Cha JH, Kim YJ, Jun WJ et al.. (2009) Epigallocatechin-3-gallate, a histone acetyltransferase inhibitor, inhibits EBV-induced B lymphocyte transformation via suppression of RelA acetylation. Cancer Res.69 (2): 583-92. [PMID:19147572]

6. Filippakopoulos P, Picaud S, Mangos M, Keates T, Lambert JP, Barsyte-Lovejoy D, Felletar I, Volkmer R, Müller S, Pawson T et al.. (2012) Histone recognition and large-scale structural analysis of the human bromodomain family. Cell149 (1): 214-31. [PMID:22464331]

7. Gallenkamp D, Gelato KA, Haendler B, Weinmann H. (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem9 (3): 438-64. [PMID:24497428]

8. Lau OD, Kundu TK, Soccio RE, Ait-Si-Ali S, Khalil EM, Vassilev A, Wolffe AP, Nakatani Y, Roeder RG, Cole PA. (2000) HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol. Cell5 (3): 589-95. [PMID:10882143]

9. Ravindra KC, Selvi BR, Arif M, Reddy BA, Thanuja GR, Agrawal S, Pradhan SK, Nagashayana N, Dasgupta D, Kundu TK. (2009) Inhibition of lysine acetyltransferase KAT3B/p300 activity by a naturally occurring hydroxynaphthoquinone, plumbagin. J. Biol. Chem.284 (36): 24453-64. [PMID:19570987]

10. SGC. I-CBP112 - a CREBBP/EP300-selective chemical probe. Accessed on 03/03/2015. Modified on 03/03/2015. thesgc.org, http://www.thesgc.org/chemical-probes/ICBP112

How to cite this page

Non-enzymatic BRD containing proteins: E1A binding protein p300. Last modified on 13/02/2017. Accessed on 11/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2735.