Actions of a picomolar short-acting S1P1 agonist in S1P1-eGFP knock-in mice

被引：71

作者：

Cahalan, Stuart M. ^{[1
,2
]}

Gonzalez-Cabrera, Pedro J. ^{[1
]}

Sarkisyan, Gor ^{[2
]}

Nhan Nguyen ^{[1
]}

Schaeffer, Marie-Therese ^{[1
]}

Huang, Liming ^{[3
]}

Yeager, Adam ^{[3
]}

Clemons, Bryan ^{[3
]}

Scott, Fiona ^{[3
]}

Rosen, Hugh ^{[1
,2
]}

机构：

[1] Scripps Res Inst, Dept Physiol Chem, La Jolla, CA 92037 USA

[2] Scripps Res Inst, Dept Immunol, La Jolla, CA 92037 USA

[3] Receptos Pharmaceut Inc, La Jolla, CA USA

来源：

NATURE CHEMICAL BIOLOGY | 2011年 / 7卷 / 05期

基金：

美国国家卫生研究院;

关键词：

SPHINGOSINE 1-PHOSPHATE RECEPTOR; PROTEIN-COUPLED RECEPTOR; ORAL FINGOLIMOD FTY720; LYMPHOCYTE EGRESS; T-CELLS; CONTROLLED-TRIAL; PHASE-II; SPHINGOSINE-1-PHOSPHATE; ACTIVATION; EDG-1;

D O I：

10.1038/nchembio.547

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

Sphingosine 1-phosphate receptor 1 (S1P(1)) is critical for lymphocyte recirculation and is a clinical target for treatment of multiple sclerosis. By generating a short-duration S1P(1) agonist and mice in which fluorescently tagged S1P(1) replaces wild-type receptor, we elucidate physiological and agonist-perturbed changes in expression of S1P(1) at a subcellular level in vivo. We demonstrate differential downregulation of S1P(1) on lymphocytes and endothelia after agonist treatment.

引用

页码：254 / 256

页数：3

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