Abstract
A new series of N-carboxyphenylpyrrole ligands were designed using GeometryFit based on an X-ray crystal structure of gp41. The synthesized ligands showed significant inhibitory activities against HIV gp41 6-helix bundle formation, HIV-1 mediated cell-cell fusion and HIV-1 replication.
Copyright 2009 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacology
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Binding Sites
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Crystallography, X-Ray
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Drug Design
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HIV Envelope Protein gp41 / chemistry*
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HIV Envelope Protein gp41 / metabolism
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HIV Fusion Inhibitors / chemical synthesis*
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HIV Fusion Inhibitors / chemistry
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HIV Fusion Inhibitors / pharmacology
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Humans
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Protein Binding
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Protein Structure, Secondary
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Pyrroles / chemical synthesis
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Pyrroles / chemistry*
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Pyrroles / pharmacology
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Thermodynamics
Substances
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Anti-HIV Agents
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HIV Envelope Protein gp41
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HIV Fusion Inhibitors
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Pyrroles