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Bioorg Med Chem Lett. 2013 Dec 1;23(23):6377-89. doi: 10.1016/j.bmcl.2013.09.058. Epub 2013 Sep 29.

Modulators of the Sphingosine 1-phosphate receptor 1.

Author information

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

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

PMID:
24125884
PMCID:
PMC3926431
DOI:
10.1016/j.bmcl.2013.09.058
[Indexed for MEDLINE]
Free PMC Article
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