2. Academic Validation
  3. Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate

Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate

  • J Med Chem. 2006 Aug 10;49(16):4809-12. doi: 10.1021/jm060554y.
Takayoshi Suzuki 1,  Akiyasu Kouketsu,  Yukihiro Itoh,  Shinya Hisakawa,  Satoko Maeda,  Minoru Yoshida,  Hidehiko Nakagawa,  Naoki Miyata
Affiliations

Affiliation

  • 1 Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Nagoya, Aichi 467-8603, Japan. suzuki@phar.nagoya-cu.ac.jp
PMID: 16884291 DOI: 10.1021/jm060554y
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-123699
    HDAC6 抑制剂
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