Ligand-binding pocket shape differences between sphingosine 1-phosphate (S1P) receptors S1P1 and S1P3 determine efficiency of chemical probe identification by ultrahigh-throughput screening.

@article{Schrer2008LigandbindingPS,
  title={Ligand-binding pocket shape differences between sphingosine 1-phosphate (S1P) receptors S1P1 and S1P3 determine efficiency of chemical probe identification by ultrahigh-throughput screening.},
  author={Stephan C. Sch{\"u}rer and Steven J. Brown and Pedro J. Gonzalez-Cabrera and M E Schaeffer and Jacqueline V. Chapman and Euijung Jo and Peter Chase and Tim S Spicer and Peter Hodder and H. K. Rosen},
  journal={ACS chemical biology},
  year={2008},
  volume={3 8},
  pages={486-98}
}
We have studied the sphingosine 1-phosphate (S1P) receptor system to better understand why certain molecular targets within a closely related family are much more tractable when identifying compelling chemical leads. Five medically important G-protein-coupled receptors for S1P regulate heart rate, coronary artery caliber, endothelial barrier integrity, and lymphocyte trafficking. Selective S1P receptor agonist probes would be of great utility to study receptor subtype-specific function. Through… CONTINUE READING