靶向gp120或gp41的小分子HIV进入抑制剂的研究进展  

Small molecule HIV entry inhibitors targeting gp120 or gp41:research advances

作　　者：代玉 田士军 何小羊 于飞[1] DAI Yu;TIAN Shi-jun;HE Xiao-yang;YU Fei(College of Life Sciences,Agricultural University of Hebei,Baoding 071000,China;Institute of Radiation Medicine,Academy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850,China)

机构地区：[1]河北农业大学生命科学学院,保定071000 [2]军事科学院军事医学研究院辐射医学研究所,北京100850

出　　处：《国际药学研究杂志》2020年第9期688-697,共10页Journal of International Pharmaceutical Research

基　　金：河北省高等学校科学技术研究项目(BJ2018045);河北省引进留学人员资助项目(CN201707)。

摘　　要：人免疫缺陷病毒Ⅰ型(HIV-1)包膜糖蛋白表面亚基gp120和跨膜亚基gp41在HIV-1进入靶细胞的过程中具有重要作用,是HIV-1进入抑制剂的关键靶位点。肽类HIV进入抑制剂(如T20)由于不能口服,导致其临床应用受限。小分子化合物具有可口服、生物利用度高等优点,是HIV进入抑制剂的重要研究方向之一。本文综述了近年来小分子HIV-1进入抑制剂的研究进展,如靶向gp120的小分子抑制剂NBD系列、BMS系列等,以及靶向gp41的小分子抑制剂NB-206、ADS-J1等,这些都是很有前景和研究价值的化合物,为设计更高效、更合理的小分子抑制剂奠定了结构基础,并发挥重要指导性作用。The envelope glycoprotein subunit gp120 and the transmembrane subunit gp41 of human immunodeficiency virus type 1(HIV-1)play important roles in the process of viral entry into target cells,and serve as key targets for developing HIV-1 entry inhibitors.Peptide HIV entry inhibitors,such as T20,are limited in clinical application due to the lack of oral properties.However,because of the possible oral administration and high bioavailability,small molecule compounds become more and more important in the research for HIV entry inhibitors.In this review,we summarize the recent advances in the development of small molecule HIV-1 entry inhibitors,including the NBD and BMS series of small-molecule inhibitors targeting gp120 as well as the NB-206 and ADS-J1 se⁃ries of small-molecule inhibitors targeting gp41.These small molecule inhibitors are promising compounds with research value,which lay a foundation for the design of more efficient and more reasonable small-molecule HIV-1 entry inhibitors.

关 键 词：人免疫缺陷病毒Ⅰ型 进入抑制剂 GP120 GP41 

分 类 号：R916[医药卫生—药学]