Highly Potent and Selective Histone Deacetylase 6 Inhibitors Designed Based on a Small-Molecular Substrate
Journal of Medicinal Chemistry2006Vol. 49(16), pp. 4809–4812
Citations Over TimeTop 10% of 2006 papers
Takayoshi Suzuki, Akiyasu Kouketsu, Yukihiro Itoh, Shinya Hisakawa, Satoko Maeda, Minoru Yoshida, Hidehiko Nakagawa, Naoki Miyata
Abstract
To find novel histone deacetylase 6 (HDAC6)-selective inhibitors and clarify the structural requirements for HDAC6-selective inhibition, we prepared thiolate analogues designed based on the structure of an HDAC6-selective substrate and evaluated the histone/alpha-tubulin acetylation selectivity by Western blot analysis. Aliphatic compounds 17b-20b selectively caused alpha-tubulin acetylation over histone H4 acetylation. In enzyme assays using HDAC1, HDAC4, and HDAC6, compounds 17a-19a exhibited HDAC6-selective inhibition over HDAC1 and HDAC4.
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