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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Antagonists of IAP Proteins: Novel Anti-Tumor Agents

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

Volume 21, Issue 34, 2014

Page: [3877 - 3892] Pages: 16

DOI: 10.2174/0929867321666140826115258

Price: $65


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.

Keywords: Antagonist, apoptosis, AVPI, IAPs, leukemia, Smac.

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