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Inside Cover: Monitoring Binding of HIV‐1 Capsid Assembly Inhibitors Using 19 F Ligand‐and 15 N Protein‐Based NMR and X‐ray Crystallography: Early Hit Validation of a Benzodiazepine Series (ChemMedChem 3/2013)
Author(s) -
Goudreau Nathalie,
Coulombe René,
Faucher AnneMarie,
GrandMaître Chantal,
Lacoste JeanEric,
Lemke Christopher T.,
Malenfant Eric,
Bousquet Yves,
Fader Lee,
Simoneau Bruno,
Mercier JeanFrançois,
Titolo Steve,
Mason Stephen W.
Publication year - 2013
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201390006
Subject(s) - capsid , crystallography , x ray , chemistry , x ray crystallography , ligand (biochemistry) , human immunodeficiency virus (hiv) , cover (algebra) , stereochemistry , diffraction , physics , biology , receptor , biochemistry , virology , quantum mechanics , optics , gene , mechanical engineering , engineering
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 19 F NMR and X‐ray co‐crystallography. For more details, see the Full Paper by Nathalie Goudreau, René Coulombe et al. on p. 405 ff.