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