G蛋白偶联受体
鞘氨醇-1-磷酸受体
鞘氨醇
受体
鞘脂
信号转导
S1PR1型
配体(生物化学)
细胞生物学
化学
突变
1-磷酸鞘氨醇
生物
生物化学
突变
癌症研究
血管内皮生长因子受体
血管内皮生长因子A
血管内皮生长因子
基因
作者
Michael A. Hanson,Christopher B. Roth,Euijung Jo,Mark T. Griffith,Fiona L. Scott,Greg J. Reinhart,Hans Desale,Bryan Clemons,Stuart M. Cahalan,Stephan C. Schuerer,Marta Sanna,Gye Won Han,Peter Kühn,Hugh Rosen,Raymond C. Stevens
出处
期刊:Science
[American Association for the Advancement of Science (AAAS)]
日期:2012-02-17
卷期号:335 (6070): 851-855
被引量:609
标识
DOI:10.1126/science.1215904
摘要
A Lipid-Sensing GPCR Sphingosine 1-phosphate (S1P) is a sphingolipid that binds to the G protein–coupled receptor subtype 1 (S1P 1 ) to activate signaling pathways involved in regulation of the vascular and immune systems. Hanson et al. (p. 851 ) determined the crystal structure of S1PR in complex with an antagonist sphingolipid mimic. Ligand access to the receptor from the extracellular milieu is occluded, and a gap between helices I and VII may provide ligand access from within the membrane. The structural information, together with mutagenesis and structure activity relationship data, provides insight into the molecular recognition events that modulate signaling.
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