Development of Small-molecule HIV Entry Inhibitors Specifically Targeting gp120 or gp41

Author(s): Lu Lu, Fei Yu, Lifeng Cai, Asim K. Debnath, Shibo Jiang

Journal Name: Current Topics in Medicinal Chemistry

Volume 16 , Issue 10 , 2016

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Graphical Abstract:


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.

Keywords: HIV, Viral entry, Entry Inhibitor, gp120, gp41.

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Article Details

Year: 2016
Published on: 09 December, 2015
Page: [1074 - 1090]
Pages: 17
DOI: 10.2174/1568026615666150901114527
Price: $65

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