title: Molecular signatures of G-protein-coupled receptors.
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.
authors: MRC Laboratory of Molecular Biology, Hills Road, Cambridge CB2 0QH, UK. ajv@mrc-lmb.cam.ac.uk
authors: A J
authors: AJ
authors: Venkatakrishnan
authors: Xavier
authors: X
authors: Deupi
authors: Guillaume
authors: G
authors: Lebon
authors: Christopher G
authors: CG
authors: Tate
authors: Gebhard F
authors: GF
authors: Schertler
authors: M Madan
authors: MM
authors: Babu
mesh_terms: D000818:Animals; D001665:Binding Sites; D018360:Crystallography, X-Ray; D006801:Humans; D008024:Ligands; D011487:Protein Conformation; D017510:Protein Folding; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled