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BioAssay: AID 392681

Inhibition of human histone acetyltransferase GCN5 in U937 cell nuclear extracts assessed as remaining enzyme activity at 50 uM

We identified a series of 4-hydroxyquinolines bearing a C1 to C15 alkyl chain at the C2 position and a carbethoxy/carboxy group at the C3 position of the quinoline nucleus (MC compounds), endowed with selective inhibitory activity against the p300/CBP HAT enzymes. Enzyme inhibition was investigated using in vitro HAT assays and by western blot analysis of cellular lysates to examine the acetylation levels of histone H3 and alpha-tubulin. When tested in U937 cells, some compounds displayed pro-apoptotic or cytodifferentiating properties. ..more
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 Tested Compounds
 Tested Compounds
All(10)
 
 
Unspecified(10)
 
 
 Tested Substances
 Tested Substances
All(10)
 
 
Unspecified(10)
 
 
 Related BioAssays
 Related BioAssays
AID: 392681
Data Source: ChEMBL (540710)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-16

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Histone acetyltransferase KAT2A; AltName: Full=General control of amino acid synthesis protein 5-like 2; AltName: Full=Histone acetyltransferase GCN5; Short=HsGCN5; AltName: Full=Lysine acetyltransferase 2A; AltName: Full=STAF97
Description ..   
Protein Family: PCAF (P300/CBP-associated factor) N-terminal domain
Comment ..   

Gene:KAT2A     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases.

Abstract: We identified a series of 4-hydroxyquinolines bearing a C1 to C15 alkyl chain at the C2 position and a carbethoxy/carboxy group at the C3 position of the quinoline nucleus (MC compounds), endowed with selective inhibitory activity against the p300/CBP HAT enzymes. Enzyme inhibition was investigated using in vitro HAT assays and by western blot analysis of cellular lysates to examine the acetylation levels of histone H3 and alpha-tubulin. When tested in U937 cells, some compounds displayed pro-apoptotic or cytodifferentiating properties.
(PMID: 19144517)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

Data Table (Concise)
Classification
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