| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372798 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
We report the systematic rational design and synthesis of new monovalent Smac mimetics that bind preferentially to the BIR2 domain of the anti-apoptotic protein XIAP. Characterization of compounds in vitro (including 9i; ML101) led to the determination of key structural requirements for BIR2 binding affinity. Compounds 9h and 9j sensitized TRAIL-resistant breast cancer cells to apoptotic cell death, highlighting the value of these probe compounds as tools to investigate the biology of XIAP.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Marcos González-Lόpez, Kate Welsh, Darren Finlay, Robert J. Ardecky, Santhi Reddy Ganji, Ying Su, Hongbin yuan, Peter Teriete, Peter D. Mace, Stefan J. Riedl, Kristiina Vuori, John C. Reed, Nicholas D.P. Cosford,