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ID: ALA1157823

Journal: Bioorg Med Chem Lett

Title: Cyclopeptide Smac mimetics as antagonists of IAP proteins.

Authors: Sun H, Liu L, Lu J, Qiu S, Yang CY, Yi H, Wang S.

Abstract: Two cyclopeptidic Smac mimetics, 2 and 3, were designed and synthesized. These two compounds bind to XIAP and cIAP-1/2 with low nanomolar affinities, and restore the activities of caspase-9 and caspase-3/-7 inhibited by XIAP. Compound 2 potently inhibits cancer cell growth and is 5-8 times more potent than the initial lead compound.

CiteXplore: 20443226

DOI: 10.1016/j.bmcl.2010.03.114