Molecular signatures of G-protein-coupled receptors
Top Cited Papers
- 13 February 2013
- journal article
- review article
- Published by Springer Science and Business Media LLC in Nature
- Vol. 494 (7436), 185-194
- https://doi.org/10.1038/nature11896
Abstract
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that sense signalling molecules such as hormones and neurotransmitters, and are the targets of several prescribed drugs. Recent exciting developments are providing unprecedented insights into the structure and function of several medically important GPCRs. Here, through a systematic analysis of high-resolution GPCR structures, we uncover a conserved network of non-covalent contacts that defines the GPCR fold. Furthermore, our comparative analysis reveals characteristic features of ligand binding and conformational changes during receptor activation. A holistic understanding that integrates molecular and systems biology of GPCRs holds promise for new therapeutics and personalized medicine.Keywords
This publication has 103 references indexed in Scilit:
- Crystal Structures of a Stabilized β1-Adrenoceptor Bound to the Biased Agonists Bucindolol and CarvedilolStructure, 2012
- Domain coupling in GPCRs: the engine for induced conformational changesTrends in Pharmacological Sciences, 2012
- A novel evolutionarily conserved domain of cell-adhesion GPCRs mediates autoproteolysisThe EMBO Journal, 2012
- Diversity and modularity of G protein-coupled receptor structuresTrends in Pharmacological Sciences, 2012
- Discovery of 1,2,4-Triazine Derivatives as Adenosine A2A Antagonists using Structure Based Drug DesignJournal of Medicinal Chemistry, 2012
- Ligand-Dependent Perturbation of the Conformational Ensemble for the GPCR β2 Adrenergic Receptor Revealed by HDXStructure, 2011
- Conformational Dynamics of Single G Protein-Coupled Receptors in SolutionThe Journal of Physical Chemistry B, 2011
- Escaping the flatlands: new approaches for studying the dynamic assembly and activation of GPCR signaling complexesTrends in Pharmacological Sciences, 2011
- Progress in Structure Based Drug Design for G Protein-Coupled ReceptorsJournal of Medicinal Chemistry, 2011
- Structural and functional protein network analyses predict novel signaling functions for rhodopsinMolecular Systems Biology, 2011