title: Modulators of the Sphingosine 1-phosphate receptor 1.
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.
authors.affiliation: Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States.
authors.forename: Mariangela
authors.initials: M
authors.lastname: Urbano
authors.forename: Miguel
authors.initials: M
authors.lastname: Guerrero
authors.forename: Hugh
authors.initials: H
authors.lastname: Rosen
authors.forename: Edward
authors.initials: E
authors.lastname: Roberts
mesh_terms: D000818:Animals; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000494:pharmacology*; D049349:Receptors, Lysosphingolipid / Q000737:chemistry / Q000378:metabolism*; D015398:Signal Transduction; D013329:Structure-Activity Relationship
chemical_list: D007166:Immunosuppressive Agents; D049349:Receptors, Lysosphingolipid
keywords: Autoimmune diseases; FTY720; S1P(1)-R agonists; S1P(1)-R antagonists