Modulators of the Sphingosine 1-phosphate receptor 1

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6377-89. doi: 10.1016/j.bmcl.2013.09.058.

Mariangela Urbano ¹, Miguel Guerrero, Hugh Rosen, Edward Roberts

Affiliations

Affiliation

1 Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States.

PMID: 24125884 DOI: 10.1016/j.bmcl.2013.09.058

Abstract

The Sphingosine 1-phosphate receptor (S1P-R) signaling system has proven to be of biological and medical importance in autoimmune settings. S1P1-R is a validated drug target for multiple sclerosis (MS) for which FTY720 (Fingolimod), a S1P1,3-5-R pan-agonist, was recently approved as the first orally active drug for the treatment of relapsing-remitting MS. Transient bradycardia and long half-life are the FTY720 critical pitfalls. This review provides the latest advances on next-generation S1P1-R modulators from 2012 up to date, with an overview of the chemical structures, structure-activity relationships, and relevant biological and clinical properties.

Keywords

Autoimmune diseases; FTY720; S1P(1)-R agonists; S1P(1)-R antagonists.

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