September 2022 "The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different subtypes of S1P receptors (S1PRs) - S1P1-5. Several S1PR therapeutic drugs have been developed to treat these diseases; however, they lack receptor Together with previously published S1PR structures in complex with antagonists and agonists, our structure of the inverse agonism in the S1PR family."

Industry News Trevena Enrolls First Subject in TRV045 Proof-of-Concept Trial Evaluating S1PR Mechanism

It is classified into two types: Sigma-1 (S1R) and Sigma-2 (S2R) based on their biological functions. S1R has been implicated in many neurological disorders such as anxiety, schizophrenia, and depression Therefore, S1R ligands possess a variety of potential clinical applications with a great interest in In this study, we report the discovery of a novel lead compound for S1R binding, based on the thiazolidine different sizes on both sides of the five-membered ring scaffold guided by the crystal structure of S1R

and Immunology A virally encoded GPCR drives glioblastoma through feed-forward activation of the SK1-S1P1