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Drug Design for G‐Protein‐Coupled Receptors by a Ligand‐Based NMR Method
Author(s) -
Bartoschek Stefan,
Klabunde Thomas,
Defossa Elisabeth,
Dietrich Viktoria,
Stengelin Siegfried,
Griesinger Christian,
Carlomagno Teresa,
Focken Ingo,
Wendt K. Ulrich
Publication year - 2010
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200905102
Subject(s) - ligand (biochemistry) , chemistry , receptor , drug discovery , combinatorial chemistry , drug , orientation (vector space) , computational biology , stereochemistry , biochemistry , biology , pharmacology , mathematics , geometry
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.