Smac mimetics as IAP antagonists. (March 2015)

• Record Type: Journal Article
• Authors: Fulda, Simone
• Is Part Of: Seminars in cell & developmental biology. Volume 39(2015)
• Page Start: 132
• Page End: 138
• Publication Date: 2015-03
• Subjects: Smac mimetic -- IAP proteins -- Cell death -- Cancer; Cytology -- Periodicals; Developmental biology -- Periodicals; 571.6
• DOI: 10.1016/j.semcdb.2014.12.005
• Languages: English
• ISSNs: 1084-9521

Abstract

Abstract: As the Inhibitor of Apoptosis (IAP) proteins are expressed at high levels in human cancers, they represent promising targets for therapeutic intervention. Small-molecule inhibitors of IAP proteins mimicking the endogenous IAP antagonist Smac, called Smac mimetics, neutralize IAP proteins and thereby promote the induction of cell death. Smac mimetics have been shown in preclinical models of human cancer to directly trigger cancer cell death or to sensitize for cancer cell death induced by a variety of cytotoxic stimuli. Smac mimetics are currently undergoing clinical evaluation in phase I/II trials, demonstrating that therapeutic targeting of IAP proteins has reached the clinical stage.