Linked Life Data

20004576

Source:http://linkedlifedata.com/resource/pubmed/id/20004576

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SubjectPredicateObjectContext
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pubmed-article:20004576pubmed:abstractTextThe ectodomain of HIV-1 gp41 mediates the fusion of viral and host cellular membranes. The peptide-based drug Enfuvirtide(1) 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 3-41microM. 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.lld:pubmed
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pubmed-article:20004576pubmed:copyrightInfoCopyright 2009 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:20004576pubmed:articleTitleNon-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket.lld:pubmed
pubmed-article:20004576pubmed:affiliationPharmaceutical Discovery Division, Abbott Laboratories, 100 Abbott Park Rd., R46Y, AP10, Abbott Park, IL 60064-6098, United States. kent.d.stewart@abbott.comlld:pubmed
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