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Actions of a picomolar short-acting S1P? agonist in S1P?-eGFP knock-in mice.


ABSTRACT: 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.

SUBMITTER: Cahalan SM 

PROVIDER: S-EPMC3430385 | biostudies-literature | 2011 May

REPOSITORIES: biostudies-literature

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

Cahalan Stuart M SM   Gonzalez-Cabrera Pedro J PJ   Sarkisyan Gor G   Nguyen Nhan N   Schaeffer Marie-Therese MT   Huang Liming L   Yeager Adam A   Clemons Bryan B   Scott Fiona F   Rosen Hugh H  

Nature chemical biology 20110327 5


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. ...[more]

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