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

  • Nat Chem Biol. 2011 May;7(5):254-6. doi: 10.1038/nchembio.547.
Stuart M Cahalan  1 ,  Pedro J Gonzalez-Cabrera ,  Gor Sarkisyan ,  Nhan Nguyen ,  Marie-Therese Schaeffer ,  Liming Huang ,  Adam Yeager ,  Bryan Clemons ,  Fiona Scott ,  Hugh Rosen
Affiliations
  • 1. Department of Chemical Physiology, The Scripps Research Institute, La Jolla, California, USA.
PMID: 21445057 DOI: 10.1038/nchembio.547
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.

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