Synthesis and evaluation of peptidic irreversible inhibitors of tissue transglutaminase

C Pardin, SMFG Gillet, JW Keillor

Index: Pardin, Christophe; Gillet, Steve M.F.G.; Keillor, Jeffrey W. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 24 p. 8379 - 8385

Full Text: HTML

Citation Number: 30

Abstract

Herein we report the synthesis and the evaluation of eight novel compounds as irreversible inhibitors of transglutaminase (TGase). These compounds are based on a minimal peptidic scaffold shown previously [Chem. Biol. 2005, 12, 469–475] to confer affinity for the TGase active site and bear electrophilic groups such as α, β-unsaturated amide, chloroacetamide or maleimide; their general structure being Cbz-Phe-spacer-electrophile. The affinity ...