An update on sphingosine-1-phosphate receptor 1 modulators

Alexander Marciniak, Sara M. Camp, Joe G.N. Garcia, Robin Polt

Research output: Contribution to journalReview articlepeer-review

24 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)3585-3591
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Issue number23-24
StatePublished - Dec 15 2018


  • Autoimmune modulators
  • S1P agonists
  • Sphingolipids
  • Sphingosine-1-phosphate
  • Sphingosine-1-phosphate receptor 1

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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