Drug Design for G-Protein-Coupled Receptors by a Ligand-Based NMR Method

A nonradioactive binding assay relying on NMR methods has been devised for a G‐protein‐coupled receptor; in addition the INPHARMA methods give access to the relative orientation of multiple ligands and supports ligand‐based drug design (see picture of superimposed ligands). The method is fast and do...

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Bibliographic Details
Published in:Angewandte Chemie (International ed.) 2010-02, Vol.49 (8), p.1426-1429
Main Authors: Bartoschek, Stefan, Klabunde, Thomas, Defossa, Elisabeth, Dietrich, Viktoria, Stengelin, Siegfried, Griesinger, Christian, Carlomagno, Teresa, Focken, Ingo, Wendt, K. Ulrich
Format: Article
Language:English
Subjects:
Drug Design
G-protein-coupled receptors
Ligands
Magnetic Resonance Spectroscopy - methods
Molecular Structure
NMR spectroscopy
Quantitative Structure-Activity Relationship
Receptors, G-Protein-Coupled - chemistry
structure-activity relationships
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Summary:A nonradioactive binding assay relying on NMR methods has been devised for a G‐protein‐coupled receptor; in addition the INPHARMA methods give access to the relative orientation of multiple ligands and supports ligand‐based drug design (see picture of superimposed ligands). The method is fast and does not require any structural information from protein crystal structures.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200905102