lysine acetyltransferase 2B | 2.3.1.48 Histone acetyltransferases (HATs) | IUPHAR/BPS Guide to PHARMACOLOGY

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lysine acetyltransferase 2B

Target not currently curated in GtoImmuPdb

Target id: 2737

Nomenclature: lysine acetyltransferase 2B

Family: 2.3.1.48 Histone acetyltransferases (HATs)

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 832 3p24 KAT2B lysine acetyltransferase 2B
Mouse - 813 17 C Kat2b K(lysine) acetyltransferase 2B
Rat - - 9q11 Kat2b lysine acetyltransferase 2B
Previous and Unofficial Names
GCN5 | GCN5L | PCAF | Pcaf | p300/CBP-associated factor | K(lysine) acetyltransferase 2B
Database Links
CATH/Gene3D 1.20.920.10
ChEMBL Target CHEMBL5500 (Hs)
Ensembl Gene ENSG00000114166 (Hs), ENSMUSG00000000708 (Mm), ENSRNOG00000011871 (Rn)
Entrez Gene 8850 (Hs), 18519 (Mm), 301164 (Rn)
Human Protein Atlas ENSG00000114166 (Hs)
KEGG Gene hsa:8850 (Hs), mmu:18519 (Mm), rno:301164 (Rn)
OMIM 602303 (Hs)
Pharos Q92831 (Hs)
RefSeq Nucleotide NM_003884 (Hs), NM_020005 (Mm)
RefSeq Protein NP_003875 (Hs), NP_064389 (Mm)
UniProtKB Q92831 (Hs), Q9JHD1 (Mm)
Wikipedia KAT2B (Hs)

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 Value Parameter Reference
compound 1 [PMID: 15724976] Hs Inhibition 8.3 pIC50 7
⤷ pIC50 8.3 (IC50 5.1x10-9 M) [7]
Description: ELISA assay measuring binding to the KAT2B (PCAF) bromodomain (GST-tagged protein containing amino acid residues 719-832) .
H3-CoA-20 Hs Inhibition 6.5 pIC50 4
⤷ pIC50 6.5 (IC50 3x10-7 M) [4]
garcinol Hs Inhibition 5.3 pIC50 1
⤷ pIC50 5.3 (IC50 5x10-6 M) [1]
LTK-14 Hs Inhibition 5.2 – 5.3 pIC50 5
⤷ pIC50 5.2 – 5.3 (IC50 7x10-6 – 5x10-6 M) [5]
anacardic acid Hs Inhibition 5.1 pIC50
⤷ pIC50 5.1 (IC50 8.5x10-6 M)
plumbagin Hs Inhibition <4.3 pIC50 6
⤷ pIC50 <4.3 (IC50 >5x10-5 M) [6]
epigallocatechin-3-gallate Hs Inhibition 4.2 pIC50 3
⤷ pIC50 4.2 (IC50 6x10-5 M) [3]
MB-3 ? Inhibition 4.0 pIC50 2
⤷ pIC50 4.0 (IC50 1x10-4 M) [2]
Lys-CoA Hs Inhibition 3.7 pIC50 4
⤷ pIC50 3.7 (IC50 2x10-4 M) [4]
View species-specific inhibitor tables
Immuno Process Associations
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0045652 regulation of megakaryocyte differentiation TAS
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0045652 regulation of megakaryocyte differentiation TAS
General Comments
This is a bromo-domain containing protein involved in chromatin modification.

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. Biel M, Kretsovali A, Karatzali E, Papamatheakis J, Giannis A. (2004) Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5. Angew. Chem. Int. Ed. Engl., 43 (30): 3974-6. [PMID:15274229]

3. 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]

4. 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]

5. Mantelingu K, Reddy BA, Swaminathan V, Kishore AH, Siddappa NB, Kumar GV, Nagashankar G, Natesh N, Roy S, Sadhale PP et al.. (2007) Specific inhibition of p300-HAT alters global gene expression and represses HIV replication. Chem. Biol., 14 (6): 645-57. [PMID:17584612]

6. 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]

7. Zeng L, Li J, Muller M, Yan S, Mujtaba S, Pan C, Wang Z, Zhou MM. (2005) Selective small molecules blocking HIV-1 Tat and coactivator PCAF association. J. Am. Chem. Soc., 127 (8): 2376-7. [PMID:15724976]

How to cite this page

2.3.1.48 Histone acetyltransferases (HATs): lysine acetyltransferase 2B. Last modified on 30/03/2016. Accessed on 19/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2737.