| Literature DB >> 15353805 |
Lin Li1, Ranny Mathew Thomas, Hidetaka Suzuki, Jef K De Brabander, Xiaodong Wang, Patrick G Harran.
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.Entities:
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Year: 2004 PMID： 15353805 DOI： 10.1126/science.1098231
Source DB: PubMed Journal: Science ISSN： 0036-8075 Impact factor: 47.728