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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacology*
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HIV Envelope Protein gp120 / antagonists & inhibitors
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HIV Envelope Protein gp120 / chemistry
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HIV Envelope Protein gp120 / metabolism*
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HIV Envelope Protein gp41 / antagonists & inhibitors
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HIV Envelope Protein gp41 / chemistry
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HIV Envelope Protein gp41 / metabolism*
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HIV Fusion Inhibitors / chemical synthesis
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HIV Fusion Inhibitors / chemistry
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HIV Fusion Inhibitors / pharmacology*
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HIV-1 / drug effects*
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HIV-1 / metabolism
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Humans
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Small Molecule Libraries / chemical synthesis
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Small Molecule Libraries / chemistry
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Small Molecule Libraries / pharmacology*
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Virus Internalization / drug effects*
Substances
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Anti-HIV Agents
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HIV Envelope Protein gp120
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HIV Envelope Protein gp41
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HIV Fusion Inhibitors
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Small Molecule Libraries