Modulators of the Sphingosine 1-phosphate receptor 1 |
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| Authors: | Mariangela Urbano Miguel Guerrero Hugh Rosen Edward Roberts |
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| Affiliation: | 1. Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States;2. Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States;3. The Scripps Research Institute, Molecular Screening Center, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States;4. Department of Immunology, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States |
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| 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. |
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| Keywords: | FTY720 Autoimmune diseases |
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