Recent Agents Targeting HIF-1α for Cancer Therapy
Recent Agents Targeting HIF-1α for Cancer Therapy
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DOI：
10.1002/jcb.24390
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发表时间：
2013-03-01
影响因子：
4
通讯作者：
Huang, He
中科院分区：
文献类型：
--
作者：
Hu, Yaozhong;Liu, Jing;Huang, He
低氧诱导因子-1（hypoxia-inducible factor-1，HIF-1）的发现使人们对肿瘤缺氧机制的认识不断加深。HIF-1作为一种重要的转录调节因子，通过激活靶基因的转录，在肿瘤细胞适应缺氧环境中发挥重要作用，调节血管生成、细胞增殖、存活、糖代谢和迁移等多种生物学过程。HIF-1抑制剂的研究为肿瘤的靶向治疗提供了新的思路。本文就缺氧诱导因子-1的生物学特性及其氧依赖性调节机制的研究进展作一综述。此外，还包括许多化学抑制剂以及蛋白质和核酸抑制剂，并主要根据其不同的抑制作用机制进行分类。我们也倾向于讨论蛋白质和核酸抑制剂与化学抑制剂相比的优势。J.细胞。114：498509，2013. (C)2012 Wiley Periodicals，Inc.
The discovery of hypoxia-inducible factor-1 (HIF-1) has led to an increasing understanding of the mechanism of tumor hypoxia in the past two decades. As a key transcriptional regulator, HIF-1 plays a central role in the adaptation of tumor cells to hypoxia by activating the transcription of targeting genes, which regulate several biological processes including angiogenesis, cell proliferation, survival, glucose metabolism and migration. The inhibitors of HIF-1 in cancer have provided us a new clue for the targeting cancer therapy. This review will introduce the general knowledge of the biology characteristic of HIF-1 and mechanism of O2-dependent regulation. Moreover, a number of chemical inhibitors plus protein and nucleic acid inhibitors are included and classified mainly based on their different mechanism of inhibiting action. We also prefer to discuss the advantages of protein and nucleic acid inhibitors compared with chemical inhibitors. J. Cell. Biochem. 114: 498509, 2013. (C) 2012 Wiley Periodicals, Inc.