缺氧(环境)
癌症研究
缺氧诱导因子
转移
医学
肿瘤微环境
癌症
肿瘤缺氧
药理学
生物
肿瘤细胞
化学
内科学
放射治疗
生物化学
基因
有机化学
氧气
作者
Hsu Feng Lu,Miao He,Minjie Wei,Yan Zhu,Wenwu Liu,Yuanyuan Yan,Xiaowen Jiang,Qinbiao Wang,Yimeng Zhao
标识
DOI:10.2174/0929867329666220829095334
摘要
Abstract: Targeting the tumor microenvironment is a promising strategy to prevent metastasis, overcome acquired drug resistance, and improve the therapeutic effect. Hypoxia is one of the characteristics of the tumor microenvironment, which is mainly regulated by hypoxia-inducible factors. Hypoxia-inducible factors (HIFs) including HIF-1α, HIF-2α, and HIF-3α, of which HIF-2α has assumed a more important role in tumor hypoxia environment. It has been demonstrated that HIF-2α plays an important role in tumor diseases, including renal cell carcinoma, breast cancer, non-small cell lung cancer, and gastric cancer, among others. Therefore, targeting HIF-2α has become one of the important strategies for treating cancers. HIF-2α inhibitors can be divided into two categories: specific inhibitors and non-specific inhibitors. The former includes synthetic monomer compounds and traditional Chinese medicine extracts. In this review, we summarized, classified, and discussed current research on the structure, structure-activity relationship (SAR), and pharmacology of HIF-2α inhibitors, which is helpful to the rational design of effective drugs for various types of malignant tumors.
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