Thermodynamic Characterization of New Positive Allosteric Modulators Binding to the Glutamate Receptor A2 Ligand-Binding Domain: Combining Experimental and Computational Methods Unravels Differences in Driving Forces

Abstract

Positive allosteric modulation of the ionotropic glutamate receptor GluA2 presents a potential treatment of cognitive disorders, for example, Alzheimer's disease. In the present study, we describe the synthesis, pharmacology, and thermodynamic studies of a series of monofluoro-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides. Measurements of… (More)
DOI: 10.1021/ci500559b

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@article{Nrholm2014ThermodynamicCO, title={Thermodynamic Characterization of New Positive Allosteric Modulators Binding to the Glutamate Receptor A2 Ligand-Binding Domain: Combining Experimental and Computational Methods Unravels Differences in Driving Forces}, author={Ann-Beth N\orholm and Pierre Francotte and Eric Goffin and Iuliana Botez and Laurence Danober and Pierre Lestage and Bernard Pirotte and Jette Sandholm Kastrup and Lars Olsen and Chris Oostenbrink}, journal={Journal of chemical information and modeling}, year={2014}, volume={54 12}, pages={3404-16} }