Tetrahedron letters

Design and synthesis of a potent biotinylated Smac mimetic

H Sun, Z Nikolovska-Coleska, CY Yang, S Wang

Index: Sun, Haiying; Nikolovska-Coleska, Zaneta; Yang, Chao-Yie; Wang, Shaomeng Tetrahedron Letters, 2005 , vol. 46, # 41 p. 7015 - 7018

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Citation Number: 9

Abstract

A biotinylated Smac mimetic () was designed based upon our previously reported potent, conformationally constrained Smac mimetic (). Smac mimetic () was synthesized and determined to bind to XIAP protein with a high-affinity (Ki value of 13nM) and is therefore a useful pharmacological tool for probing the intracellular targets of this class of potent Smac mimetics.