tailieunhanh - Báo cáo khoa học: NMR structure of the thromboxane A2 receptor ligand recognition pocket

Toovercome the difficultyof characterizing the structures of the extracellular loops (eLPs) ofGprotein-coupledreceptors (GPCRs) other than rhodopsin, we have explored a strategy to generate a three-dimensional structural model for a GPCR, the thromboxane A2 receptor. This three-dimen-sional structurewas completedby the assembly of theNMR structures of the computation-guided constrained peptides that mimicked the extracellular loops and connected to the conserved seven transmembrane domains. | Eur. J. Biochem. 271 3006-3016 2004 FEBS 2004 doi NMR structure of the thromboxane A2 receptor ligand recognition pocket Ke-He Ruan Jiaxin Wu Shui-Ping So Lori A. Jenkins and Cheng-Huai Ruan Vascular Biology Research Center and Division of Hematology Department of Internal Medicine The University of Texas Health Science Center Houston TX USA To overcome the difficulty of characterizing the structures of the extracellular loops eLPs of G protein-coupled receptors GPCRs other than rhodopsin we have explored a strategy to generate a three-dimensional structural model for a GPCR the thromboxane A2 receptor. This three-dimensional structure was completed by the assembly of the NMR structures of the computation-guided constrained peptides that mimicked the extracellular loops and connected to the conserved seven transmembrane domains. The NMR structure-based model reveals the structural features of the eLPs in which the second extracellular loop eLP2 and the disulfide bond between the first extracellular loop eLP1 and eLP2 play a major role in forming the ligand recognition pocket. The eLP2 conformation is dynamic and regulated by the oxidation and reduction of the disulfide bond which affects ligand docking in the initial recognition. The reduced form of the thromboxane A2 receptor experienced a decrease in ligand binding activity due to the rearrangement of the eLP2 conformation. The ligand-bound receptor was however resistant to the reduction inactivation because the ligand covered the disulfide bond and stabilized the eLP2 conformation. This molecular mechanism of ligand recognition is the first that may be applied to other prostanoid receptors and other GPCRs. Keywords G protein-coupled receptor thromboxane A2 thromboxane A2 receptor NMR synthetic peptide. Prostanoids comprising prostaglandins and thromboxane A2 act as local hormones in the vicinity of their production site to regulate hemostasis and smooth muscle function. These .

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