H3-CoA-20   Click here for help

GtoPdb Ligand ID: 7035

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].
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1. Cole PA. (2008)
Chemical probes for histone-modifying enzymes.
Nat Chem Biol, 4 (10): 590-7. [PMID:18800048]
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]
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]