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Binding of Ligands to GPCRs – How Valid is a Thermodynamic
Discrimination of Antagonists and Agonists?

URN to cite this document:
Strasser, Andrea ; Wittmann, Hans-Joachim
License: Creative Commons: Attribution 3.0
PDF - Published Version
Date of publication of this fulltext: 12 Feb 2014 10:25


Abstract In 1979, a thermodynamic discrimination between antagonists and agonists at GPCRs was discussed in literature for the first time. Subsequently a small number of experimental studies, addressing not only Gibbs energy but also enthalpy and entropy of ligand binding were performed within the last 30 years at different GPCRs. Some of these studies support the suggested “thermodynamic ...


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