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. 2004 Aug 12;47(17):4147-50.
doi: 10.1021/jm0499108.

Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site

Haiying Sun  1 , Zaneta Nikolovska-Coleska, Chao-Yie Yang, Liang Xu, York Tomita, Krzysztof Krajewski, Peter P Roller, Shaomeng Wang
Affiliations

Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site

Haiying Sun et al. J Med Chem. .

Abstract

A successful structure-based design of conformationally constrained second mitochondria-derived activator of caspase (Smac) mimetics that target the XIAP/caspase-9 interaction site is described. The most potent Smac mimetic 12d has a Ki of 350 nM for binding to the XIAP BIR3 domain protein. 12d is found to be effective in enhancing apoptosis induced by cisplatin in PC-3 human prostate cancer cells.

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