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Compound class:
Peptide or derivative
Comment: This compound is a member of a new class of histone acetyltransferase inhibitors known as bisubstrate inhibitors. It is formed from coenzyme A modified with peptide side chains of histone H3 sequence. See Lau et al (2000) for structural details [2]. The 3 dimensional structure of this compound in complex with GCN5 histone acetyltransferase (KAT2A) has been published [3]. For a review of compounds being investigated as modulators of histone-modifying enzyme activity see [1].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Cole PA. (2008)
Chemical probes for histone-modifying enzymes. Nat Chem Biol, 4 (10): 590-7. [PMID:18800048] |
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2. 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] |
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3. Poux AN, Cebrat M, Kim CM, Cole PA, Marmorstein R. (2002)
Structure of the GCN5 histone acetyltransferase bound to a bisubstrate inhibitor. Proc Natl Acad Sci USA, 99 (22): 14065-70. [PMID:12391296] |
