3V2Y

Crystal Structure of a Lipid G protein-Coupled Receptor at 2.80A

3V2Y の概要

• エントリーDOI: 10.2210/pdb3v2y/pdb
• 関連するPDBエントリー: 3v2w
• 分子名称: Sphingosine 1-phosphate receptor 1, Lysozyme chimera (E.C.3.2.1.17), {(3R)-3-amino-4-[(3-hexylphenyl)amino]-4-oxobutyl}phosphonic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... (4 entities in total)
• 機能のキーワード: sphingosine, edg receptor, lipid receptor, multiple sclerosis, autoimmunity, structural genomics, psi-biology, gpcr network, gpcr, membrane protein, g protein coupled receptor, membrane, 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: 59536.75

構造登録者

Hanson, M.A.,Roth, C.B.,Jo, E.,Griffith, M.T.,Scott, F.L.,Reinhart, G.,Desale, H.,Clemons, B.,Cahalan, S.M.,Schuerer, S.C.,Sanna, M.G.,Han, G.W.,Kuhn, P.,Rosen, H.,Stevens, R.C.,GPCR Network (GPCR) (登録日: 2011-12-12, 公開日: 2012-02-15, 最終更新日: 2024-04-03)

主引用文献

Hanson, M.A.,Roth, C.B.,Jo, E.,Griffith, M.T.,Scott, F.L.,Reinhart, G.,Desale, H.,Clemons, B.,Cahalan, S.M.,Schuerer, S.C.,Sanna, M.G.,Han, G.W.,Kuhn, P.,Rosen, H.,Stevens, R.C.
Crystal structure of a lipid G protein-coupled receptor.
Science, 335:851-855, 2012

PubMed Abstract: The lyso-phospholipid sphingosine 1-phosphate modulates lymphocyte trafficking, endothelial development and integrity, heart rate, and vascular tone and maturation by activating G protein-coupled sphingosine 1-phosphate receptors. Here, we present the crystal structure of the sphingosine 1-phosphate receptor 1 fused to T4-lysozyme (S1P(1)-T4L) in complex with an antagonist sphingolipid mimic. Extracellular access to the binding pocket is occluded by the amino terminus and extracellular loops of the receptor. Access is gained by ligands entering laterally between helices I and VII within the transmembrane region of the receptor. This structure, along with mutagenesis, agonist structure-activity relationship data, and modeling, provides a detailed view of the molecular recognition and requirement for hydrophobic volume that activates S1P(1), resulting in the modulation of immune and stromal cell responses.

PubMed: 22344443
DOI: 10.1126/science.1215904

実験手法

X-RAY DIFFRACTION (2.8 Å)