Subtype selective substrates for histone deacetylases

…, M Yoshida, N Nishino, E Verdin, M Jung

Index: Heltweg, Birgit; Dequiedt, Franck; Marshall, Brett L.; Brauch, Carsten; Yoshida, Minoru; Nishino, Norikazu; Verdin, Eric; Jung, Manfred Journal of Medicinal Chemistry, 2004 , vol. 47, # 21 p. 5235 - 5243

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Citation Number: 111

Abstract

To probe the steric requirements for deacylation, we synthesized lysine-derived small molecule substrates and examined structure-reactivity relationships with various histone deacetylases. Rat liver, human HeLa, and human recombinant class I and II histone deacetylases (HDACs) as well as human recombinant NAD+-dependent SIRT1 (class III enzyme) were used in these studies. A benzyloxycarbonyl substituent on the α-amino ...