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BioAssay: AID 602819

Inhibition of histone acetylase activity of human recombinant PCAF expressed in Escherichia coli at 50 uM using biotinylated oligopeptide sequences from histone H3 (1-21) substrate by In-vitro time-resolved fluorescence immunosorbent acetyltransferase assay

We present a combination of database screening, synthesis and in vitro testing to identify novel histone acetyltransferase (HAT) inhibitors. The National Cancer Institute compound collection (NCI) and several commercial databases were filtered by similarity-based virtual screening to find new HAT inhibitors. Employing the recombinant HAT p300/CBP-associated factor (PCAF) and two different histone more ..
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 Tested Compounds
 Tested Compounds
All(7)
 
 
Unspecified(7)
 
 
 Tested Substances
 Tested Substances
All(7)
 
 
Unspecified(7)
 
 
 Related BioAssays
 Related BioAssays
AID: 602819
Data Source: ChEMBL (752829)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-05-25

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Histone acetyltransferase KAT2B; AltName: Full=Histone acetyltransferase PCAF; Short=Histone acetylase PCAF; AltName: Full=Lysine acetyltransferase 2B; AltName: Full=P300/CBP-associated factor; Short=P/CAF
Description ..   
Protein Family: PCAF (P300/CBP-associated factor) N-terminal domain
Comment ..   

Gene:KAT2B     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Synthesis and biological testing of novel pyridoisothiazolones as histone acetyltransferase inhibitors.

Abstract: We present a combination of database screening, synthesis and in vitro testing to identify novel histone acetyltransferase (HAT) inhibitors. The National Cancer Institute compound collection (NCI) and several commercial databases were filtered by similarity-based virtual screening to find new HAT inhibitors. Employing the recombinant HAT p300/CBP-associated factor (PCAF) and two different histone substrates for screening, pyridoisothiazolones were identified as inhibitors of human PCAF. Due to the limited solubility of the initial hits, we synthesized and tested them on PCAF. The compounds inhibit the proliferation of cancer cells. In summary, valuable chemical tools and potential lead candidates for new anticancer agents directed against HATs as new targets have been identified.
(PMID: 21353783)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

Data Table (Concise)
Classification
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