title: Proton transfer-mediated GPCR activation.
abstract: G-protein coupled receptors (GPCRs) play essential roles in signal transduction from the environment into the cell. While many structural features have been elucidated in great detail, a common functional mechanism on how the ligand-binding signal is converted into a conformational change on the cytoplasmic face resulting in subsequent activation of downstream effectors remain to be established. Based on available structural and functional data of the activation process in class-A GPCRs, we propose here that a change in protonation status, together with proton transfer via conserved structural elements located in the transmembrane region, are the key elements essential for signal transduction across the membrane.
authors.affiliation: National Laboratory of Macromolecules, National Center of Protein Science-Beijing, Institute of Biophysics, Chinese Academy of Sciences, Beijing, 100101, China, zhangc@ibp.ac.cn.
authors.forename: Xuejun C
authors.initials: XC
authors.lastname: Zhang
authors.forename: Can
authors.initials: C
authors.lastname: Cao
authors.forename: Ye
authors.initials: Y
authors.lastname: Zhou
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D020816:Amino Acid Motifs; D006801:Humans; D008564:Membrane Potentials; D008565:Membrane Proteins / Q000737:chemistry / Q000378:metabolism; D011522:Protons; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D008565:Membrane Proteins; D011522:Protons; D043562:Receptors, G-Protein-Coupled