Inside Cover: Monitoring Binding of HIV-1 Capsid Assembly Inhibitors Using 19F Ligand-and 15N Protein-Based NMR and X-ray Crystallography: Early Hit Validation of a Benzodiazepine Series (ChemMedChem 3/2013)

Authors

  • Dr. Nathalie Goudreau,

    Corresponding author
    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
    • Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • René Coulombe,

    Corresponding author
    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
    • Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Dr. Anne-Marie Faucher,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
    2. Department of Chemistry, University of Montreal, C.P. 6128, succursale Centre-ville, Montreal, Québec, H3C 3J7 (Canada)
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  • Chantal Grand-Maître,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Jean-Eric Lacoste,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Dr. Christopher T. Lemke,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Eric Malenfant,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Yves Bousquet,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Dr. Lee Fader,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Dr. Bruno Simoneau,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Jean-François Mercier,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
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  • Steve Titolo,

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
    2. AL-G Technologies Inc. 201 Mgr. Bourget, Lévis, Québec, G6V 9V6 (Canada)
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  • Dr. Stephen W. Mason

    1. Dept. of Chemistry and Biological Sciences, Research & Development, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, H7S 2G5 (Canada)
    2. Virology, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492 (USA)
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Abstract

original image

Mature HIV-1 capsid (CA) core is characterized by a fullerene cone-shaped structure made of hexamers and pentamers. Inhibition of its assembly is a novel mechanism through which to target HIV-1. The inside cover picture shows the characterization of potent CA assembly inhibitors (orange) as N-terminal domain (NTD) binders using 19F NMR and X-ray co-crystallography. For more details, see the Full Paper by Nathalie Goudreau, René Coulombe et al. on p. 405 ff.

Cartoon 1.

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