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A High-throughput Cre-Lox Activated Viral Membrane Fusion Assay to Identify Inhibitors of HIV-1 Viral Membrane Fusion
Published on: August 14, 2018
A targeted covalent small molecule inhibitor of HIV-1 fusion
Guangyan Zhou1, Li He1, Kathy H Li2
1Department of Basic Sciences, Touro University California, 1310 Club Drive, Mare Island, Vallejo, CA 94592, USA. miriam.gochin@tu.edu.
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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