期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 16, 期 10, 页码 1074-1090出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026615666150901114527
关键词
HIV; Viral entry; Entry Inhibitor; gp120; gp41
资金
- Natural Science Foundation of China [81173098, 81361120378, 81373456]
- 973 program of China [2012CB519001]
- Shanghai Pujiang Program [13PJD004]
- NIH [RO1 AI104416]
- NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [R01AI104416] Funding Source: NIH RePORTER
Human immunodeficiency virus type 1 (HIV-1) envelope (Env) glycoprotein surface subunit gp120 and transmembrane subunit gp41 play important roles in HIV-1 entry, thus serving as key targets for the development of HIV-1 entry inhibitors. T20 peptide (enfuvirtide) is the first U.S. FDA-approved HIV entry inhibitor; however, its clinical application is limited by the lack of oral availability. Here, we have described the structure and function of the HIV-1 gp120 and gp41 subunits and reviewed advancements in the development of small-molecule HIV entry inhibitors specifically targeting these two Env glycoproteins. We then compared the advantages and disadvantages of different categories of HIV entry inhibitor candidates and further predicted the future trend of HIV entry inhibitor development.
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