| Literature DB >> 15603949 |
Takayoshi Suzuki1, Azusa Matsuura, Akiyasu Kouketsu, Hidehiko Nakagawa, Naoki Miyata.
Abstract
In order to find novel non-hydroxamate histone deacetylase (HDAC) inhibitors, we synthesized several suberoylanilide hydroxamic acid (SAHA)-based compounds designed on the basis of the catalytic mechanism of HDACs. Among these compounds, 5b was found to be as potent as SAHA. Kinetic enzyme assays and molecular modeling suggested that the mercaptoacetamide moiety of 5b interacts with the zinc in the active site of HDACs and removes a water molecule from the reactive site of the deacetylation.Entities:
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Year: 2005 PMID： 15603949 DOI： 10.1016/j.bmcl.2004.10.074
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823