4.5 Article

Cyclopeptide Smac mimetics as antagonists of IAP proteins

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 10, 页码 3043-3046

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.03.114

关键词

Smac mimetics; IAP antagonists; Apoptosis inducers; New anticancer agents

资金

  1. National Cancer Institute, National Institutes of Health, USA [R01CA127551, R01CA109025]

向作者/读者索取更多资源

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. (C) 2010 Published by Elsevier Ltd.

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