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
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
GO Annotations:  Associated to 1 GO processes
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS
GO:0045652 regulation of megakaryocyte differentiation TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0032481 positive regulation of type I interferon production TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS
click arrow to show/hide IEA associations
GO:0030183 B cell differentiation IEA
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0030183 B cell differentiation IEA
Immuno Process:  Immune system development
GO Annotations:  Associated to 4 GO processes, IEA only
GO:0045652 regulation of megakaryocyte differentiation TAS
click arrow to show/hide IEA associations
GO:0030183 B cell differentiation IEA
GO:0030220 platelet formation IEA
GO:0035855 megakaryocyte development IEA
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. Cell, 149 (1): 214-31. [PMID:22464331]

7. Gallenkamp D, Gelato KA, Haendler B, Weinmann H. (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem, 9 (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. Cell, 5 (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 21/06/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2735.