Target General Infomation
Target ID
T16902 (Former ID: TTDI00174)
Target Name
Histone acetyltransferase KAT2B (KAT2B)
Synonyms
Spermidine acetyltransferase KAT2B; PCAF; P300/CBP-associated factor; P/CAF; Lysine acetyltransferase 2B; Histone acetyltransferase PCAF; Histone acetylase PCAF
Gene Name
KAT2B
Target Type
Literature-reported target
[1]
Function
Has significant histone acetyltransferase activity with core histones (H3 and H4), and also with nucleosome core particles. Also acetylates non-histone proteins, such as ACLY, PLK4 and TBX5. Inhibits cell-cycle progression and counteracts the mitogenic activity of the adenoviral oncoprotein E1A. Acts as a circadian transcriptional coactivator which enhances the activity of the circadian transcriptional activators: NPAS2-ARNTL/BMAL1 and CLOCK-ARNTL/BMAL1 heterodimers. Involved in heart and limb development by mediating acetylation of TBX5, acetylation regulating nucleocytoplasmic shuttling of TBX5. Acts as a negative regulator of centrosome amplification by mediating acetylation of PLK4. Also acetylates spermidine. Functions as a histone acetyltransferase (HAT) to promote transcriptional activation.
BioChemical Class
Acyltransferase
UniProt ID
KAT2B_HUMAN
EC Number
EC 2.3.1.48
Sequence
MSEAGGAGPGGCGAGAGAGAGPGALPPQPAALPPAPPQGSPCAAAAGGSGACGPATAVAA
AGTAEGPGGGGSARIAVKKAQLRSAPRAKKLEKLGVYSACKAEESCKCNGWKNPNPSPTP
PRADLQQIIVSLTESCRSCSHALAAHVSHLENVSEEEMNRLLGIVLDVEYLFTCVHKEED
ADTKQVYFYLFKLLRKSILQRGKPVVEGSLEKKPPFEKPSIEQGVNNFVQYKFSHLPAKE
RQTIVELAKMFLNRINYWHLEAPSQRRLRSPNDDISGYKENYTRWLCYCNVPQFCDSLPR
YETTQVFGRTLLRSVFTVMRRQLLEQARQEKDKLPLEKRTLILTHFPKFLSMLEEEVYSQ
NSPIWDQDFLSASSRTSQLGIQTVINPPPVAGTISYNSTSSSLEQPNAGSSSPACKASSG
LEANPGEKRKMTDSHVLEEAKKPRVMGDIPMELINEVMSTITDPAAMLGPETNFLSAHSA
RDEAARLEERRGVIEFHVVGNSLNQKPNKKILMWLVGLQNVFSHQLPRMPKEYITRLVFD
PKHKTLALIKDGRVIGGICFRMFPSQGFTEIVFCAVTSNEQVKGYGTHLMNHLKEYHIKH
DILNFLTYADEYAIGYFKKQGFSKEIKIPKTKYVGYIKDYEGATLMGCELNPRIPYTEFS
VIIKKQKEIIKKLIERKQAQIRKVYPGLSCFKDGVRQIPIESIPGIRETGWKPSGKEKSK
EPRDPDQLYSTLKSILQQVKSHQSAWPFMEPVKRTEAPGYYEVIRFPMDLKTMSERLKNR
YYVSKKLFMADLQRVFTNCKEYNPPESEYYKCANILEKFFFSKIKEAGLIDK
Mode of Action [+] 1 Modes of Action +
Inhibitor [+] 5 Inhibitor drugs +
1 anacardic acid Drug Info [2]
2 garcinol Drug Info [3]
3 LTK-14 Drug Info [1]
4 MB-3 Drug Info [4]
5 PMID15724976C1 Drug Info [5]
Target Regulators
Target-regulating microRNAs
Target-interacting Proteins
Target Affiliated Biological Pathways
Panther Pathway [+] 1 Panther Pathways +
1 p53 pathway
PID Pathway [+] 8 PID Pathways +
1 Regulation of nuclear SMAD2/3 signaling
2 Signaling events mediated by HDAC Class III
3 E2F transcription factor network
4 Signaling events mediated by HDAC Class I
5 FoxO family signaling
6 Regulation of Androgen receptor activity
7 Retinoic acid receptors-mediated signaling
8 p53 pathway
Reactome [+] 8 Reactome Pathways +
1 Pre-NOTCH Transcription and Translation
2 YAP1- and WWTR1 (TAZ)-stimulated gene expression
3 NOTCH1 Intracellular Domain Regulates Transcription
4 Constitutive Signaling by NOTCH1 PEST Domain Mutants
5 Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
6 HATs acetylate histones
7 Notch-HLH transcription pathway
8 RNA Polymerase I Transcription Initiation
WikiPathways [+] 5 WikiPathways +
1 Nuclear Receptors Meta-Pathway
2 YAP1- and WWTR1 (TAZ)-stimulated gene expression
3 Notch Signaling Pathway
4 RNA Polymerase I, RNA Polymerase III, and Mitochondrial Transcription
5 Androgen receptor signaling pathway
References
REF 1 Specific inhibition of p300-HAT alters global gene expression and represses HIV replication. Chem Biol. 2007 Jun;14(6):645-57.
REF 2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2737).
REF 3 Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene e... J Biol Chem. 2004 Aug 6;279(32):33716-26.
REF 4 Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5. Angew Chem Int Ed Engl. 2004 Jul 26;43(30):3974-6.
REF 5 Selective small molecules blocking HIV-1 Tat and coactivator PCAF association. J Am Chem Soc. 2005 Mar 2;127(8):2376-7.

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