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

Curr Top Med Chem

Key Laboratory of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Building #13, Shanghai 200032, China.

Published: November 2016

AI Article Synopsis

  • HIV-1 envelope glycoproteins, gp120 and gp41, are crucial for the virus's entry into host cells, making them prime targets for entry inhibitors.
  • T20 peptide (enfuvirtide) is the first approved entry inhibitor but has limitations like poor oral availability.
  • The text reviews the structures and functions of gp120 and gp41, discusses advancements in small-molecule inhibitors targeting these proteins, and analyzes the pros and cons of various inhibitor candidates while predicting future development trends.

Article 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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4775441PMC
http://dx.doi.org/10.2174/1568026615666150901114527DOI Listing

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