title: Structural studies of G protein-coupled receptors.
abstract: G protein-coupled receptors (GPCRs) comprise the largest membrane protein family. These receptors sense a variety of signaling molecules, activate multiple intracellular signal pathways, and act as the targets of over 40% of marketed drugs. Recent progress on GPCR structural studies provides invaluable insights into the structure-function relationship of the GPCR superfamily, deepening our understanding about the molecular mechanisms of GPCR signal transduction. Here, we review recent breakthroughs on GPCR structure determination and the structural features of GPCRs, and take the structures of chemokine receptor CCR5 and purinergic receptors P2Y1R and P2Y12R as examples to discuss the importance of GPCR structures on functional studies and drug discovery. In addition, we discuss the prospect of GPCR structure-based drug discovery. © 2016 IUBMB Life, 68(11):894-903, 2016.
authors.affiliation: CAS Key laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.|University of Chinese Academy of Sciences, Beijing, China.
authors.forename: Mengjie
authors.initials: M
authors.lastname: Lu
authors.affiliation: CAS Key laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China. beiliwu@simm.ac.cn.|School of Life Science and Technology, ShanghaiTech University, Pudong, Shanghai, China. beiliwu@simm.ac.cn.
authors.forename: Beili
authors.initials: B
authors.lastname: Wu
mesh_terms: D001665:Binding Sites; D018360:Crystallography, X-Ray; D006801:Humans; D008958:Models, Molecular; D000072756:Protein Conformation, alpha-Helical; D000072417:Protein Domains; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000502:physiology
chemical_list: D043562:Receptors, G-Protein-Coupled
keywords: G protein-coupled receptor; chemokine receptor; purinergic receptor; structural studies