A small molecule Smac mimic potentiates TRAIL- and TNFalpha-mediated cell death - PubMed (original) (raw)
. 2004 Sep 3;305(5689):1471-4.
doi: 10.1126/science.1098231.
Affiliations
- PMID: 15353805
- DOI: 10.1126/science.1098231
A small molecule Smac mimic potentiates TRAIL- and TNFalpha-mediated cell death
Lin Li et al. Science. 2004.
Abstract
We describe the synthesis and properties of a small molecule mimic of Smac, a pro-apoptotic protein that functions by relieving inhibitor-of-apoptosis protein (IAP)-mediated suppression of caspase activity. The compound binds to X chromosome- encoded IAP (XIAP), cellular IAP 1 (cIAP-1), and cellular IAP 2 (cIAP-2) and synergizes with both tumor necrosis factor alpha (TNFalpha) and TNF-related apoptosis-inducing ligand (TRAIL) to potently induce caspase activation and apoptosis in human cancer cells. The molecule has allowed a temporal, unbiased evaluation of the roles that IAP proteins play during signaling from TRAIL and TNF receptors. The compound is also a lead structure for the development of IAP antagonists potentially useful as therapy for cancer and inflammatory diseases.
Comment in
- Medicine. Targeting apoptotic pathways in cancer cells.
Denicourt C, Dowdy SF. Denicourt C, et al. Science. 2004 Sep 3;305(5689):1411-3. doi: 10.1126/science.1102974. Science. 2004. PMID: 15353788 No abstract available.
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