Design and synthesis of a potent biotinylated Smac mimetic

作者：Sun HY; Nikolovska Coleska Z; Yang CY; Wang SM^*

来源：Tetrahedron Letters, 2005, 46(41): 7015-7018.

DOI：10.1016/j.tetlet.2005.08.055

• Smac mimetic
• biotinylated ligand
• XIAP

A biotinylated Smac mimetic (2) was designed based upon our previously reported potent, conformationally constrained Smac mimetic (1). Smac mimetic (2) was synthesized and determined to bind to XIAP protein with a high-affinity (K-i value of 13 nM) and is therefore a useful pharmacological tool for probing the intracellular targets of this class of potent Smac mimetics.

• 出版日期2005-10-10