Journal of Medicinal Chemistry 2006-11-30

Discovering inhibitors of human sirtuin type 2: novel structural scaffolds.

Anu J Tervo, Tiina Suuronen, Sergiy Kyrylenko, Erkki Kuusisto, Päivi H Kiviranta, Antero Salminen, Jukka Leppänen, Antti Poso

Index: J. Med. Chem. 49 , 7239-7241, (2006)

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Abstract

A successful virtual screening experiment of novel SIRT2 inhibitors is described. Four out of 11 experimentally tested compounds showed in vitro inhibitory activity toward SIRT2 in a micromolar level, resulting in an experimental hit ratio of 36%. Two of these compounds inhibited SIRT2 with IC50 (microM) values of 51 and 91; moreover, one of the new inhibitors was comprised of an entirely new SIRT2-inhibiting structural scaffold.