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Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic

Journal of Medicinal Chemistry, ISSN: 0022-2623, Vol: 49, Issue: 26, Page: 7916-7920
2006
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Article Description

A potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase mimetic (SM-131, 2) has been designed, synthesized, and evaluated. Compound 2 binds to X-linked inhibitors of apoptosis proteins (XIAP) with a K of 61 nM in a competitive binding assay and directly antagonizes the XIAP inhibition of caspase-9 activity in a cell-free functional assay. Compound 2 achieves an IC of 100 nM in inhibition of cell growth and effectively induces cell death in the MDA-MB-231 human breast cancer cell line. © 2006 American Chemical Society.

Bibliographic Details

Sun, Haiying; Nikolovska-Coleska, Zaneta; Lu, Jianfeng; Qiu, Su; Yang, Chao-Yie; Gao, Wei; Meagher, Jennifer; Stuckey, Jeanne; Wang, Shaomeng

American Chemical Society (ACS)

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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