2. Academic Validation
  3. Identification of novel SIRT2-selective inhibitors using a click chemistry approach

Identification of novel SIRT2-selective inhibitors using a click chemistry approach

  • Bioorg Med Chem Lett. 2014 Apr 15;24(8):1871-4. doi: 10.1016/j.bmcl.2014.03.026.
Prima R Tatum 1,  Hideyuki Sawada 2,  Yosuke Ota 2,  Yukihiro Itoh 2,  Peng Zhan 2,  Naoya Ieda 1,  Hidehiko Nakagawa 1,  Naoki Miyata 3,  Takayoshi Suzuki 4
Affiliations

Affiliations

  • 1 Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
  • 2 Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Taishogun Nishitakatsukasa-Cho, Kita-ku, Kyoto 603-8334, Japan.
  • 3 Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan. Electronic address: miyata-n@phar.nagoya-cu.ac.jp.
  • 4 Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Taishogun Nishitakatsukasa-Cho, Kita-ku, Kyoto 603-8334, Japan. Electronic address: suzukit@koto.kpu-m.ac.jp.
PMID: 24675380 DOI: 10.1016/j.bmcl.2014.03.026
Abstract

A series of 114 SIRT inhibitor candidates was assembled using 'click chemistry', by reacting two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in the presence of Cu(I) catalyst. Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT2 Inhibitor. These findings will be useful for further development of SIRT2-selective inhibitors.

Keywords

Histone deacetylase; Inhibitor; Isozyme selectivity; Sirtuin.

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