Proton transfer-mediated GPCR activation  

作　　者：Xuejun C. Zhang Can Cao Ye Zhou Yan Zhao 

机构地区：[1]National Laboratory of Macromolecules, National Center of Protein Science--Beijing, Institute of Biophysics, ChineseAcademy of Sciences, Beijing 100101, China

出　　处：《Protein & Cell》2015年第1期12-17,共6页蛋白质与细胞（英文版）

摘　　要：G-protein coupled receptors （GPCRs） play essential roles in signal transduction from the environment into the cell. While many structural features have been elu- cidated in great detail, a common functional mechanism on how the ligand-binding signal is converted into a conformational change on the cytoplasmic face result- ing 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 trans- duction across the membrane.G-protein coupled receptors （GPCRs） play essential roles in signal transduction from the environment into the cell. While many structural features have been elu- cidated in great detail, a common functional mechanism on how the ligand-binding signal is converted into a conformational change on the cytoplasmic face result- ing 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 trans- duction across the membrane.

关 键 词：GPCR ACTIVATION PROTONATION membranepotential 

分 类 号：Q51[生物学—生物化学] TN304.23[电子电信—物理电子学]