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Binding of Ligands to GPCRs – How Valid is a Thermodynamic Discrimination of Antagonists and Agonists? | OMICS International | Abstract
ISSN: 2161-0398

Journal of Physical Chemistry & Biophysics
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Review Article

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

Andrea Strasser1* and Hans-Joachim Wittmann2
1Department of Pharmaceutical/Medicinal Chemistry II, University of Regensburg, Regensburg, Germany
2Faculty of Chemistry and Pharmacy, University of Regensburg, Regensburg, Germany
Corresponding Author : Andrea Strasser
Department of Pharmaceutical/Medicinal Chemistry II
Institute of Pharmacy, University of Regensburg
Universitätsstrabe 31, D-93040 Regensburg, Germany
Tel: +49-941-943-4821
E-mail: [email protected]
Received September 18, 2012; Accepted October 19, 2012; Published October 22, 2012
Citation: Strasser A, Wittmann HJ (2012) Binding of Ligands to GPCRs – How Valid is a Thermodynamic Discrimination of Antagonists and Agonists? J Physic Chem Biophysic S1:001. doi:10.4172/2161-0398.S1-001
Copyright: © 2012 Strasser A, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.


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 discrimination”, but this concept does not hold for all GPCRs analyzed by thermodynamic methods so far. This review presents an overview in this field of research. Furthermore, the data presented in literature are critically discussed and related to each other. As experimental methods provide information about the final and the starting state of the ligand-receptor binding, specific sub-processes are not accessible. But in the framework of an interpretation on a molecular level, quantitative insights in these processes are essential. A workaround of this problem is given by the development of molecular modelling methods, during the last decade. Taking into account all data so far, the concept of “thermodynamic discrimination” between antagonists and agonists may be extended to “thermodynamic and kinetic discrimination” of antagonists, partial agonists and full agonists. However, to obtain a deeper insight on molecular level, more systematic studies, including a large number of compounds with high structural variety have to be performed.
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