1. Department of Microbiology and Molecular Genetics, University of Pittsburgh School of Medicine, Pittsburgh, PA 15219, USA;2. Department of Structural Biology, University of Pittsburgh School of Medicine, Pittsburgh, PA 15219, USA;3. Drug Discovery Institute, University of Pittsburgh School of Medicine, Pittsburgh, PA 15219, USA;4. Departments of Pharmacology and Chemistry, University of Virginia, Charlottesville, VA 22908, USA;5. Department of Pharmaceutical Sciences, University of Pittsburgh School of Pharmacy, Pittsburgh, PA 15261, USA
Abstract:
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Highlights? Nef is a critical HIV virulence factor lacking biochemical activity amenable to HTS ? HTS for inhibitors of Nef-mediated Hck kinase activation identified Nef antagonists ? Hit compound B9 blocks Nef-dependent HIV replication with submicromolar potency ? B9 binds directly to purified HIV Nef in vitro and blocks Nef dimerization in cells
