A targeted covalent small molecule inhibitor of HIV-1 fusion | Zendy

Guangyan Zhou | Zendy; Li He | Zendy; Kathy H. Li | Zendy; Cássio Cardoso Santos Pedroso | Zendy; Miriam Gochin | Zendy

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A targeted covalent small molecule inhibitor of HIV-1 fusion

Author(s) -

Guangyan Zhou,

Li He,

Kathy H. Li,

Cássio Cardoso Santos Pedroso,

Miriam Gochin

Publication year - 2021

Publication title -

chemical communications

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.837

H-Index - 333

eISSN - 1364-548X

pISSN - 1359-7345

DOI - 10.1039/d1cc01013a

Subject(s) - covalent bond , chemistry , fusion , residue (chemistry) , peptide , small molecule , glycoprotein , lysine , human immunodeficiency virus (hiv) , fusion protein , combinatorial chemistry , stereochemistry , biophysics , biochemistry , recombinant dna , biology , virology , amino acid , organic chemistry , philosophy , linguistics , gene

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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