Details of the Biological Target of DIG (DBT)
| General Information of DBT (ID: ET0I9GC) | |||||
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| Name |
Histone acetylase PCAF (KAT2B)
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| Synonyms |
Click to Show/Hide the Synonyms of This DBT
Histone acetyltransferase KAT2B; Histone acetyltransferase PCAF; Lysine acetyltransferase 2B; P/CAF; P300/CBP-associated factor; PCAF; Spermidine acetyltransferase KAT2B
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| Family | Transferase (TFase) >> Acyltransferase (EC 2.3) | ||||
| Organism |
Homo sapiens (Human)
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| Gene Name | KAT2B | Gene ID | |||
| UniProt ID | KAT2B_HUMAN | (click to find more protein-related data of this DBT) | |||
| TTD ID | T16902 | (click to find more therapeutic target data of this DBT) | |||
| Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target | |||||
| Sequence |
MSEAGGAGPGGCGAGAGAGAGPGALPPQPAALPPAPPQGSPCAAAAGGSGACGPATAVAA
AGTAEGPGGGGSARIAVKKAQLRSAPRAKKLEKLGVYSACKAEESCKCNGWKNPNPSPTP PRADLQQIIVSLTESCRSCSHALAAHVSHLENVSEEEMNRLLGIVLDVEYLFTCVHKEED ADTKQVYFYLFKLLRKSILQRGKPVVEGSLEKKPPFEKPSIEQGVNNFVQYKFSHLPAKE RQTIVELAKMFLNRINYWHLEAPSQRRLRSPNDDISGYKENYTRWLCYCNVPQFCDSLPR YETTQVFGRTLLRSVFTVMRRQLLEQARQEKDKLPLEKRTLILTHFPKFLSMLEEEVYSQ NSPIWDQDFLSASSRTSQLGIQTVINPPPVAGTISYNSTSSSLEQPNAGSSSPACKASSG LEANPGEKRKMTDSHVLEEAKKPRVMGDIPMELINEVMSTITDPAAMLGPETNFLSAHSA RDEAARLEERRGVIEFHVVGNSLNQKPNKKILMWLVGLQNVFSHQLPRMPKEYITRLVFD PKHKTLALIKDGRVIGGICFRMFPSQGFTEIVFCAVTSNEQVKGYGTHLMNHLKEYHIKH DILNFLTYADEYAIGYFKKQGFSKEIKIPKTKYVGYIKDYEGATLMGCELNPRIPYTEFS VIIKKQKEIIKKLIERKQAQIRKVYPGLSCFKDGVRQIPIESIPGIRETGWKPSGKEKSK EPRDPDQLYSTLKSILQQVKSHQSAWPFMEPVKRTEAPGYYEVIRFPMDLKTMSERLKNR YYVSKKLFMADLQRVFTNCKEYNPPESEYYKCANILEKFFFSKIKEAGLIDK |
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| 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.
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| Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT | ||||||
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| DIG Name: Methylchloroisothiazolinone | Click to Show/Hide | |||||
| Detailed Information |
DIG Info
 click to show the detail info of this DIG
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| Functional Class | Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
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| Experiment for Assessing the Biological Activity of This DIG on the Studied DBT | ||||||
| Biological Activity | IC50 = 3000 nM (estimated based on the structural similarity with CHEMBL461475 ) | [1] | ||||
| Structural Similarity | Tanimoto coefficient = 0.925 | |||||
| Tested Species | Homo sapiens (Human) | |||||
| UniProt ID | KAT2B_HUMAN | |||||
| References | |||||
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| 1 | Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase. Eur J Med Chem. 2009 Dec; 44(12):4855-61. | ||||
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