Journal
PHARMACOLOGY & THERAPEUTICS
Volume 144, Issue 1, Pages 82-95Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.pharmthera.2014.05.007
Keywords
SMAC mimetics; Apoptosis; Inhibitors
Categories
Funding
- Breast Cancer Research Foundation
- Prostate Cancer Foundation
- Department of Defense Prostate Cancer Program [W81XWH-04-1-0213]
- Ascenta Therapeutics
- Debiopharm
- National Cancer Institute, NIH [5R01CA109025, 5R01CA127551]
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Apoptosis is a tightly regulated cellular process and faulty regulation of apoptosis is a hallmark of human cancers. Targeting key apoptosis regulators with the goal to restore apoptosis in tumor cells has been pursued as a new cancer therapeutic strategy. XIAP, cIAP1, and cIAP2, members of inhibitor of apoptosis (IAP) proteins, are critical regulators of cell death and survival and are attractive targets for new cancer therapy. The SMAC/DIABLO protein is an endogenous antagonist of XIAP, cIAP1, and cIAP2. In the last decade, intense research efforts have resulted in the design and development of several small-molecule SMAC mimetics now in clinical trials for cancer treatment. In this review, we will discuss the roles of XIAP, cIAP1, and cIAP2 in regulation of cell death and survival, and the design and development of small-molecule SMAC mimetics as novel cancer treatments. (C) 2014 Elsevier Inc. All rights reserved.
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