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.
Rights & PermissionsPrintExport