Abstract
G protein-coupled receptors (GPCRs) are a large superfamily of signaling proteins expressed on the plasma membrane. They are involved in a wide range of physiological processes and, therefore, are exploited as drug targets in a multitude of therapeutic areas. In this extent, knowledge of structural and functional properties of GPCRs may greatly facilitate rational design of modulator compounds. Solution and solid-state nuclear magnetic resonance (NMR) spectroscopy represents a powerful method to gather atomistic insights into protein structure and dynamics. In spite of the difficulties inherent the solution of the structure of membrane proteins through NMR, these methods have been successfully applied, sometimes in combination with molecular modeling, to the determination of the structure of GPCR fragments, the mapping of receptor-ligand interactions, and the study of the conformational changes associated with the activation of the receptors. In this review, we provide a summary of the NMR contributions to the study of the structure and function of GPCRs, also in light of the published crystal structures.
Keywords: G protein-coupled receptors (GPCRs), NMR, three-dimensional structures, ligand recognition, receptor activation
Current Pharmaceutical Design
Title: Unraveling the Structure and Function of G Protein-Coupled Receptors Through NMR Spectroscopy
Volume: 15 Issue: 35
Author(s): Irina G. Tikhonova and Stefano Costanzi
Affiliation:
Keywords: G protein-coupled receptors (GPCRs), NMR, three-dimensional structures, ligand recognition, receptor activation
Abstract: G protein-coupled receptors (GPCRs) are a large superfamily of signaling proteins expressed on the plasma membrane. They are involved in a wide range of physiological processes and, therefore, are exploited as drug targets in a multitude of therapeutic areas. In this extent, knowledge of structural and functional properties of GPCRs may greatly facilitate rational design of modulator compounds. Solution and solid-state nuclear magnetic resonance (NMR) spectroscopy represents a powerful method to gather atomistic insights into protein structure and dynamics. In spite of the difficulties inherent the solution of the structure of membrane proteins through NMR, these methods have been successfully applied, sometimes in combination with molecular modeling, to the determination of the structure of GPCR fragments, the mapping of receptor-ligand interactions, and the study of the conformational changes associated with the activation of the receptors. In this review, we provide a summary of the NMR contributions to the study of the structure and function of GPCRs, also in light of the published crystal structures.
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Cite this article as:
Tikhonova G. Irina and Costanzi Stefano, Unraveling the Structure and Function of G Protein-Coupled Receptors Through NMR Spectroscopy, Current Pharmaceutical Design 2009; 15 (35) . https://dx.doi.org/10.2174/138161209789824803
DOI https://dx.doi.org/10.2174/138161209789824803 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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