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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
The 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.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AndersonSteveS,
pubmed-author:BarrettLeo WLW,
pubmed-author:CarrickRobertR,
pubmed-author:HutchinsonRebecca NewlinRN,
pubmed-author:HuthJeffrey RJR,
pubmed-author:KempfDale JDJ,
pubmed-author:KohlbrennerWilliamW,
pubmed-author:MaringClarenceC,
pubmed-author:MatayoshiEdmund DED,
pubmed-author:McDanielKeithK,
pubmed-author:MeadowsRobertR,
pubmed-author:MendozaRenaldo RRR,
pubmed-author:MoHongmeiH,
pubmed-author:MollaAkhterA,
pubmed-author:NgTeresa ITI,
pubmed-author:OlejniczakEdward TET,
pubmed-author:RichardsonPaul LPL,
pubmed-author:SeverinJeanJ,
pubmed-author:StewartKent DKD,
pubmed-author:StollVincent SVS,
pubmed-author:WalterKarlK
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pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
612-7
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pubmed:meshHeading |
pubmed-meshheading:20004576-Anti-HIV Agents,
pubmed-meshheading:20004576-Benzamides,
pubmed-meshheading:20004576-Crystallography, X-Ray,
pubmed-meshheading:20004576-HIV Envelope Protein gp41,
pubmed-meshheading:20004576-HIV Fusion Inhibitors,
pubmed-meshheading:20004576-Humans,
pubmed-meshheading:20004576-Magnetic Resonance Spectroscopy,
pubmed-meshheading:20004576-Models, Molecular,
pubmed-meshheading:20004576-Peptide Fragments,
pubmed-meshheading:20004576-Protein Binding,
pubmed-meshheading:20004576-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Non-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket.
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pubmed:affiliation |
Pharmaceutical Discovery Division, Abbott Laboratories, 100 Abbott Park Rd., R46Y, AP10, Abbott Park, IL 60064-6098, United States. kent.d.stewart@abbott.com
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pubmed:publicationType |
Journal Article
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