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Review
. 2022:1366:27-43.
doi: 10.1007/978-981-16-8702-0_3.

Small-Molecule HIV Entry Inhibitors Targeting gp120 and gp41

Fei Yu  1 , Shibo Jiang  2
Affiliations
Review

Small-Molecule HIV Entry Inhibitors Targeting gp120 and gp41

Fei Yu et al. Adv Exp Med Biol. 2022.

Abstract

Interrupting early events in the virus life cycle, such as those prior to the formation of provirus, could effectively prevent HIV-1 infection. HIV-1 entry into host cells is mediated by the envelope glycoprotein (Env) trimer, which is composed of three gp120 exterior glycoproteins and three gp41 transmembrane glycoproteins. Hence, the development of novel inhibitors targeting these two glycoproteins could hold the key to early inhibition of HIV-1 infection. Small-molecule entry inhibitors targeting early events in the virus life cycle comprise a well-established class of useful drugs. Many libraries of small-molecule inhibitors have been established to screen potential drug candidates for a variety of targets based on computer docking, FRET, or peptide-linked assay. This chapter reviews the mechanisms of some small-molecule inhibitors targeting HIV-1 gp120 and gp41 and corresponding high-efficiency screening strategies for potential small-molecule inhibitors.

Keywords: Mechanisms of action; Screening strategies; Small-molecule inhibitors; Virus.

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References

    1. Armand-Ugon M, Clotet-Codina I, Tintori C, Manetti F, Clotet B, Botta M, Este JA (2005) The anti-HIV activity of ADS-J1 targets the HIV-1 gp120. Virology 343(1):141–149. https://doi.org/10.1016/j.virol.2005.08.007 - DOI - PubMed
    1. Caffrey M (2001) Model for the structure of the HIV gp41 ectodomain: insight into the intermolecular interactions of the gp41 loop. BBA-Mol Basis Dis 1536(2–3):116–122. https://doi.org/10.1016/S0925-4439(01)00042-4 - DOI
    1. Cai L, Gochin M (2007) A novel fluorescence intensity screening assay identifies new low-molecular-weight inhibitors of the gp41 coiled-coil domain of human immunodeficiency virus type 1. Antimicrob Agents Chemother 51(7):2388–2395. https://doi.org/10.1128/AAC.00150-07 - DOI - PubMed - PMC
    1. Case MA, Ghadiri MR, Mutz MW, McLendon GL (1998) Stereoselection in designed three-helix bundle metalloproteins. Chirality 10(1–2):35–40. https://doi.org/10.1002/chir.7 - DOI - PubMed
    1. Chan DC, Kim PS (1998) HIV entry and its inhibition. Cell 93(5):681–684. https://doi.org/10.1016/S0092-8674(00)81430-0 - DOI - PubMed

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