Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design

T Suzuki, A Matsuura, A Kouketsu, H Nakagawa…

文献索引：Suzuki, Takayoshi; Matsuura, Azusa; Kouketsu, Akiyasu; Nakagawa, Hidehiko; Miyata, Naoki Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 2 p. 331 - 335

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被引用次数: 66

摘要

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 ...