Monday, April 5, 2021

A targeted covalent small molecule inhibitor of HIV-1 fusion

Guangyan Zhou Li He Kathy H Li Cassio Cardoso Santos Pedroso and Miriam Gochin

Chem. Commun., 2021

DOI: 10.1039/D1CC01013A 

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 inhibitor.

Thiol Reactivity of N-Aryl α-Methylene-γ-lactams: Influence of the Guaianolide Structure [@KayBrummond]

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