An update on sphingosine-1-phosphate receptor 1 modulators |
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Authors: | Alexander Marciniak Sara M. Camp Joe G.N. Garcia Robin Polt |
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Affiliation: | 1. Department of Chemistry & Biochemistry, The University of Arizona, Tucson, AZ 85721, United States;2. Department of Medicine, The University of Arizona, Tucson, AZ 85724, United States |
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Abstract: | Sphingolipids represent an essential class of lipids found in all eukaryotes, and strongly influence cellular signal transduction. Autoimmune diseases like asthma and multiple sclerosis (MS) are mediated by the sphingosine-1-phosphate receptor 1 (S1P1) to express a variety of symptoms and disease patterns. Inspired by its natural substrate, an array of artificial sphingolipid derivatives has been developed to target this specific G protein-coupled receptor (GPCR) in an attempt to suppress autoimmune disorders. FTY720, also known as fingolimod, is the first oral disease-modifying therapy for MS on the market. In pursuit of improved stability, bioavailability, and efficiency, structural analogues of this initial prodrug have emerged over time. This review covers a brief introduction to the sphingolipid metabolism, the mechanism of action on S1P1, and an updated overview of synthetic sphingosine S1P1 agonists. |
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Keywords: | Sphingolipids Sphingosine-1-phosphate Sphingosine-1-phosphate receptor 1 Autoimmune modulators Corresponding author. |
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