Article
Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants.
Scientific reports - 11 Sept 2015
Harpsøe Kasper, Isberg Vignir, Tehan Benjamin G, Weiss Dahlia, Arsova Angela, Marshall Fiona H, Bräuner-Osborne Hans, Gloriam David E
Abstract excerpt
The metabotropic glutamate receptors have a wide range of modulatory functions in the central nervous system. They are among the most highly pursued drug targets, with relevance for several neurological diseases, and a number of allosteric modulators have entered clinical trials. However, so far this has not led to a marketed drug, largely because of the difficulties in achieving subtype-selective compounds with...
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