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• W1964364336 abstract "The ectodomain of HIV-1 gp41 mediates the fusion of viral and host cellular membranes. The peptide-based drug Enfuvirtide1 is precedent that antagonists of this fusion activity may act as anti HIV-agents. Here, NMR screening was used to discover non-peptide leads against this target and resulted in the discovery of a new benzamide 1 series. This series is non-peptide, low molecular weight, and analogs have activity in a cell fusion assay with EC50 values ranging 3–41 μM. Structural work on the gp41/benzamide 1 complex was determined by NMR spectroscopy using a designed model peptide system that mimics an open pocket of the fusogenic form of the protein." @default.
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• W1964364336 date "2010-01-01" @default.
• W1964364336 modified "2023-10-10" @default.
• W1964364336 title "Non-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket" @default.
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• W1964364336 doi "https://doi.org/10.1016/j.bmcl.2009.11.076" @default.
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