Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 26, Pages 7916-7920Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm061108d
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Funding
- NCI NIH HHS [R01 CA 109025, P30 CA 046592] Funding Source: Medline
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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-i 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 IC50 of 100 nM in inhibition of cell growth and effectively induces cell death in the MDA-MB-231 human breast cancer cell line.
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