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靶向HIF-1α/p300蛋白-蛋白相互作用抑制剂的研究进展

莫小飞, 徐晓莉, 王亚楼, 尤启冬

莫小飞, 徐晓莉, 王亚楼, 尤启冬. 靶向HIF-1α/p300蛋白-蛋白相互作用抑制剂的研究进展[J]. 中国药科大学学报, 2017, 48(5): 515-522. DOI: 10.11665/j.issn.1000-5048.20170502
引用本文: 莫小飞, 徐晓莉, 王亚楼, 尤启冬. 靶向HIF-1α/p300蛋白-蛋白相互作用抑制剂的研究进展[J]. 中国药科大学学报, 2017, 48(5): 515-522. DOI: 10.11665/j.issn.1000-5048.20170502
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MO Xiaofei, XU Xiaoli, WANG Yalou, YOU Qidong. Advances in the HIF-1α/p300 protein-protein interaction inhibitors[J]. Journal of China Pharmaceutical University, 2017, 48(5): 515-522. DOI: 10.11665/j.issn.1000-5048.20170502
Citation: MO Xiaofei, XU Xiaoli, WANG Yalou, YOU Qidong. Advances in the HIF-1α/p300 protein-protein interaction inhibitors[J]. Journal of China Pharmaceutical University, 2017, 48(5): 515-522. DOI: 10.11665/j.issn.1000-5048.20170502
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靶向HIF-1α/p300蛋白-蛋白相互作用抑制剂的研究进展

  • 1.

    中国药科大学江苏省药物分子设计与成药性优化重点实验室

  • 2.

    中国药科大学药物化学系

基金项目: 国家自然科学基金资助项目(NO.81502990,No.81573346)；江苏省自然科学基金资助项目(No.BK20150691)

Advances in the HIF-1α/p300 protein-protein interaction inhibitors

摘要

    摘要
  • 摘要: 缺氧诱导因子-1α(hypoxia induced factor-1α，HIF-1α)是肿瘤适应缺氧微环境的重要调节因子。它调控细胞增殖与存活、新陈代谢、血管生成、入侵与转移等相关行为的100多个靶基因，而HIF-1α/p300是调控这些下游基因表达的重要复合物，靶向HIF-1α/p300蛋白-蛋白相互作用展开抑制剂的开发成为抗肿瘤药物研究的又一热点。本文对HIF-1α信号通路、HIF-1α/p300蛋白-蛋白相互作用的结合模式以及近年HIF-1α/p300蛋白-蛋白相互作用抑制剂的研究进展进行了综述，为该类抑制剂的设计提供参考。
    Abstract: Hypoxia induced factor-1α(HIF-1α)is a key regulation factor that helps tumor adapt itself to the hypoxia microenvironment. It regulates the expression of more than 100 target genes that control cell proliferation and survival, metabolism, angiogenesis, invasion and metastasis. HIF-1α/p300, a core complex that regulates downstream genes expression, is considered as a potential antitumor target. This review summarizes HIF-1α signal pathway, the binding mode of HIF-1α/p300 protein-protein interaction and recent development on the HIF-1α/p300 protein-protein interaction inhibitors, which provides reference to the design of this kind of inhibitors.
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    • 参考文献(30)
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  • 刊出日期:  2017-10-24

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