Fulda S
Institute for Experimental Cancer Research in Pediatrics, Goethe-University, Frankfurt, Germany; German Cancer Consortium (DKTK), Heidelberg, Germany; German Cancer Research Center (DKFZ), Heidelberg, Germany.
Int Rev Cell Mol Biol. 2017;330:157-169. doi: 10.1016/bs.ircmb.2016.09.004. Epub 2017 Jan 23.
Inhibitor of Apoptosis (IAP) proteins are overexpressed in a variety of human cancers. Therefore, they are considered as promising targets for the design of therapeutic strategies. Smac mimetics mimic the endogenous mitochondrial protein Smac that antagonizes IAP proteins upon its release into the cytosol. Multiple preclinical studies have documented the ability of Smac mimetics to either directly induce cell death of cancer cells or to prime them to agents that trigger cell death. At present, several Smac mimetics are being evaluated in early clinical trials. The current review provides an overview on the potential of Smac mimetics as cancer therapeutics to target IAP proteins for cancer therapy.
凋亡抑制蛋白（IAP）在多种人类癌症中过度表达。因此，它们被视为设计治疗策略的有前景的靶点。Smac模拟物模仿内源性线粒体蛋白Smac，后者在释放到细胞质中时可拮抗IAP蛋白。多项临床前研究已证明Smac模拟物能够直接诱导癌细胞死亡或使癌细胞对触发细胞死亡的药物敏感。目前，几种Smac模拟物正在早期临床试验中进行评估。本综述概述了Smac模拟物作为癌症治疗药物靶向IAP蛋白用于癌症治疗的潜力。
