IAP蛋白的拮抗剂：新型抗肿瘤剂

Title:Antagonists of IAP Proteins: Novel Anti-Tumor Agents

Volume: 21 Issue: 34

Author(s): Yichao Wan, Tingting Liu, Xuben Hou, Yanyan Dun, Peng Guan and Hao Fang

Affiliation:

关键词: 拮抗剂、细胞凋亡、丙氨酸-缬氨酸-脯氨酸-异亮氨酸 、凋亡抑制蛋白 、白血病 、半胱天冬酶第二线粒体源性激活剂

摘要: Evasion of apoptosis is an important reason for tumor cells to resist the anticancer drugs in cancer therapy. As a critical regulator, the inhibitor of apoptosis proteins (IAPs) can block the apoptosis by inhibiting the activities of caspases. Scientists find that IAPs are over-expressed in many cancer cells, such as leukemia and B-cell lymphoma, which elucidate that high levels of IAPs are closely related to tumorigenesis and cancer development. Thus, targeting IAPs may be an attractive strategy for anti-tumor treatment. As an endogenous antagonist of IAPs, second mitochondria-derived activator of caspases (Smac) can suppress their activities through directly binding to IAPs. Based on structural biology study, Smac interacts with IAPs through the Ala-Val-Pro-Ile (AVPI) tetra-peptide of Smac. Therefore, many agents have been studied to suppress the IAPs which result in the activation of caspases and subsequently induce the apoptosis of tumor cells based on mimicking AVPI peptide strategy. In this review, the functions of IAPs in apoptosis and the recent advance of IAPs antagonists will be discussed.

Cite this article as:

Wan Yichao, Liu Tingting, Hou Xuben, Dun Yanyan, Guan Peng and Fang Hao, Antagonists of IAP Proteins: Novel Anti-Tumor Agents, Current Medicinal Chemistry 2014; 21 (34) . https://dx.doi.org/10.2174/0929867321666140826115258