2RH1

High resolution crystal structure of human B2-adrenergic G protein-coupled receptor.

2RH1 の概要

• エントリーDOI: 10.2210/pdb2rh1/pdb
• 関連するBIRD辞書のPRD_ID: PRD_900001
• 分子名称: beta-2-adrenergic receptor/T4-lysozyme chimera, alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose, SULFATE ION, ... (10 entities in total)
• 機能のキーワード: gpcr, 7tm, adrenergic, fusion, lipidic cubic phase, lipidic, mesophase, cholesterol, membrane protein, membrane protein - hydrolase complex, structural genomics, psi-2, protein structure initiative, accelerated technologies center for gene to 3d structure, atcg3d, gpcr network, membrane protein / hydrolase
• 由来する生物種: Homo sapiens (human,); 詳細
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 60020.83

構造登録者

Cherezov, V.,Rosenbaum, D.M.,Hanson, M.A.,Rasmussen, S.G.F.,Thian, F.S.,Kobilka, T.S.,Choi, H.J.,Kuhn, P.,Weis, W.I.,Kobilka, B.K.,Stevens, R.C.,Accelerated Technologies Center for Gene to 3D Structure (ATCG3D),GPCR Network (GPCR) (登録日: 2007-10-05, 公開日: 2007-10-30, 最終更新日: 2024-10-30)

主引用文献

Cherezov, V.,Rosenbaum, D.M.,Hanson, M.A.,Rasmussen, S.G.,Thian, F.S.,Kobilka, T.S.,Choi, H.J.,Kuhn, P.,Weis, W.I.,Kobilka, B.K.,Stevens, R.C.
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor.
Science, 318:1258-1265, 2007

PubMed Abstract: Heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors constitute the largest family of eukaryotic signal transduction proteins that communicate across the membrane. We report the crystal structure of a human beta2-adrenergic receptor-T4 lysozyme fusion protein bound to the partial inverse agonist carazolol at 2.4 angstrom resolution. The structure provides a high-resolution view of a human G protein-coupled receptor bound to a diffusible ligand. Ligand-binding site accessibility is enabled by the second extracellular loop, which is held out of the binding cavity by a pair of closely spaced disulfide bridges and a short helical segment within the loop. Cholesterol, a necessary component for crystallization, mediates an intriguing parallel association of receptor molecules in the crystal lattice. Although the location of carazolol in the beta2-adrenergic receptor is very similar to that of retinal in rhodopsin, structural differences in the ligand-binding site and other regions highlight the challenges in using rhodopsin as a template model for this large receptor family.

PubMed: 17962520
DOI: 10.1126/science.1150577

実験手法

X-RAY DIFFRACTION (2.4 Å)