The structure and function of the S1P1 receptor.

摘要: Sphingosine 1-phosphate (S1P) receptors (S1PRs) belong to the class A family of G protein-coupled (GPCRs). S1PRs are widely expressed on many cell types, including those immune, cardiovascular, and central nervous systems. The S1PR is rapidly gaining attention as an important mediator cellular processes, differentiation, migration, survival, angiogenesis, calcium homeostasis, inflammation immunity. Importantly, known drug targets for multiple sclerosis (MS), which newly developed oral therapy fingolimod, modulator, has recently been approved clinical use. Much progress also made in field structural biology modeling heterotrimeric GPCRs allowing crystal structure S1PR1 subtype be elucidated key interactions defined. Here, we outline function S1PR1, highlighting residues involved receptor activation, signaling, transmembrane interactions, ligand binding, post-translational modification, protein–protein interactions.