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Updated: Jun 15, 2026

A High-throughput Cre-Lox Activated Viral Membrane Fusion Assay to Identify Inhibitors of HIV-1 Viral Membrane Fusion
Published on: August 14, 2018
[Integrase inhibitor, CCR5 antagonist, fusion inhibitor]
1AIDS Clinical Center, International Medical Center of Japan.
Abstract:
Integrase inhibitors have a novel antiretroviral mechanism which prevents proviral DNA integration into the CD4+ cell chromosome. Promising results have been seen in clinical trials in treatment-naïve and -experienced infected individuals. CCR5 antagonists bind to CCR5, one of the second receptors of HIV-1, and inhibit HIV-1 entry into CD4+ cells. However, they cannot prevent the cell entry of HIV-1s which can use another second receptor, CXCR4. Fusion inhibitors are synthetic peptides which mimic a fragment of HIV-1 gp41. They can bind a counterpart portion of HIV-1 gp41 and prevent the fusion of viral and cellular membranes, one of the critical steps of HIV-1 entry into CD4+ cells.
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