Article
S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate.
Chemistry & biology - 1 Jun 2005
Jo Euijung, Sanna M Germana, Gonzalez-Cabrera Pedro J, Thangada Shobha, Tigyi Gabor, Osborne Daniel A, Hla Timothy, Parrill Abby L, Rosen Hugh
Abstract excerpt
The essential role of the sphingosine 1-phosphate (S1P) receptor S1P(1) in regulating lymphocyte trafficking was demonstrated with the S1P(1)-selective nanomolar agonist, SEW2871. Despite its lack of charged headgroup, the tetraaromatic compound SEW2871 binds and activates S1P(1) through a combination of hydrophobic and ion-dipole interactions. Both S1P and SEW2871 activated ERK, Akt, and Rac signaling pathways...
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