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核心蛋白变构调节剂的研究进展

高倩倩, 韩开林, 王国成, 陆涛

高倩倩, 韩开林, 王国成, 陆涛. 核心蛋白变构调节剂的研究进展[J]. 中国药科大学学报, 2019, 50(5): 516-522. DOI: 10.11665/j.issn.1000-5048.20190502
引用本文: 高倩倩, 韩开林, 王国成, 陆涛. 核心蛋白变构调节剂的研究进展[J]. 中国药科大学学报, 2019, 50(5): 516-522. DOI: 10.11665/j.issn.1000-5048.20190502
GAO Qianqian, HAN Kailin, WANG Guocheng, LU Tao. Advances in core protein allosteric modulators[J]. Journal of China Pharmaceutical University, 2019, 50(5): 516-522. DOI: 10.11665/j.issn.1000-5048.20190502
Citation: GAO Qianqian, HAN Kailin, WANG Guocheng, LU Tao. Advances in core protein allosteric modulators[J]. Journal of China Pharmaceutical University, 2019, 50(5): 516-522. DOI: 10.11665/j.issn.1000-5048.20190502

核心蛋白变构调节剂的研究进展

Advances in core protein allosteric modulators

  • 摘要: 核心蛋白变构调节剂以核心蛋白为靶点,通过调控共价闭合环状DNA(cccDNA)的形成来抑制乙型肝炎病毒(HBV)复制,有望用于乙型肝炎治疗并克服核苷类药物的耐药问题。本文从HBV的复制过程、核心蛋白的功能、核心蛋白变构调节剂的作用机制、分类及临床研究进展等方面进行综述,列举了12个该类药物,并总结了其机制、所属类别、化学结构、安全性、抗HBV效果、联合用药情况等,此外探讨了核心蛋白变构调节剂的优势及存在的问题,期望能为抗HBV的新药开发提供参考。
    Abstract: The core protein allosteric modulator targets the core protein and inhibits hepatitis B virus(HBV)replication by regulating the formation of covalently closed circular DNA(cccDNA), which is expected to completely cure hepatitis B and overcome the drug resistance of nucleoside drugs. This paper reviews the replication process of HBV, the function of core proteins, the mechanism, classification and research progress of core protein allosteric modulators, lists 12 drugs, and summarizes their mechanisms, categories, chemical structures, safety, anti-HBV effects, combined drug use, etc. In addition, the advantages and problems of core protein allosteric modulators are discussed to provide references for the development of new anti-HBV drugs.
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出版历程
  • 刊出日期:  2019-10-24

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