3D4S

Cholesterol bound form of human beta2 adrenergic receptor.

3D4S の概要

• エントリーDOI: 10.2210/pdb3d4s/pdb
• 関連するPDBエントリー: 2RH1
• 分子名称: Beta-2 adrenergic receptor/T4-lysozyme chimera, (2S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol, CHOLESTEROL, ... (5 entities in total)
• 機能のキーワード: gpcr, membrane protein, lysozyme, fusion, adrenergic, timolol, g-protein coupled receptor, glycoprotein, lipoprotein, palmitate, phosphoprotein, receptor, transducer, transmembrane, structural genomics, psi-2, protein structure initiative, accelerated technologies center for gene to 3d structure, atcg3d, gpcr network
• 由来する生物種: Homo sapiens; 詳細
• 細胞内の位置: Cell membrane ; Multi- pass membrane protein : P07550
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 58117.27

構造登録者

Hanson, M.A.,Cherezov, V.,Roth, C.B.,Griffith, M.T.,Jaakola, V.-P.,Chien, E.Y.T.,Velasquez, J.,Kuhn, P.,Stevens, R.C.,Accelerated Technologies Center for Gene to 3D Structure (ATCG3D),GPCR Network (GPCR) (登録日: 2008-05-14, 公開日: 2008-06-17, 最終更新日: 2024-10-30)

主引用文献

Hanson, M.A.,Cherezov, V.,Griffith, M.T.,Roth, C.B.,Jaakola, V.P.,Chien, E.Y.,Velasquez, J.,Kuhn, P.,Stevens, R.C.
A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor.
Structure, 16:897-905, 2008

PubMed Abstract: The role of cholesterol in eukaryotic membrane protein function has been attributed primarily to an influence on membrane fluidity and curvature. We present the 2.8 A resolution crystal structure of a thermally stabilized human beta(2)-adrenergic receptor bound to cholesterol and the partial inverse agonist timolol. The receptors pack as monomers in an antiparallel association with two distinct cholesterol molecules bound per receptor, but not in the packing interface, thereby indicating a structurally relevant cholesterol-binding site between helices I, II, III, and IV. Thermal stability analysis using isothermal denaturation confirms that a cholesterol analog significantly enhances the stability of the receptor. A consensus motif is defined that predicts cholesterol binding for 44% of human class A receptors, suggesting that specific sterol binding is important to the structure and stability of other G protein-coupled receptors, and that this site may provide a target for therapeutic discovery.

PubMed: 18547522
DOI: 10.1016/j.str.2008.05.001

実験手法

X-RAY DIFFRACTION (2.8 Å)