A Targeted Covalent Small Molecule Inhibitor of HIV-1 Fusion

Overview

Journal Chem Commun (Camb)

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2021 May 6

PMID 33956029

Citations 2

Authors

Guangyan Zhou

Li He

Kathy H Li

Cassio C S Pedroso

Miriam Gochin

Affiliations

Soon will be listed here.

Abstract

We describe a low molecular weight covalent inhibitor targeting a conserved lysine residue within the hydrophobic pocket of HIV-1 glycoprotein-41. The inhibitor bound selectively to the hydrophobic pocket and exhibited an order of magnitude enhancement of anti-fusion activity against HIV-1 compared to its non-covalent counterpart. The findings represent a significant advance in the quest to obtain non-peptide fusion inhibitors.

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