A targeted covalent small molecule inhibitor of HIV-1 fusion.
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ABSTRACT:
SUBMITTER: Zhou G
PROVIDER: S-EPMC8141304 | biostudies-literature | 2021 May
REPOSITORIES: biostudies-literature
Publications
A targeted covalent small molecule inhibitor of HIV-1 fusion.
Zhou Guangyan G He Li L Li Kathy H KH Pedroso Cássio C S CCS Gochin Miriam M
Chemical communications (Cambridge, England) 20210501 37
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. ...[more]
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