S1PR1 binds S1PR1 agonists

Stable Identifier
Reaction [binding]
Homo sapiens
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Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid that regulates a diverse range of physiological processes such as lymphocyte trafficking, cardiac function, vascular development, and inflammation. S1P receptor 1 (S1PR1) agonists possess immunomodulatory/immunosuppresant actions. The S1PR1 agonists fingolimod (FTY720) (Chun & Hartung 2010), siponimod (BAF312) (Pan et al. 2013, Glaenzel et al. 2018) and ozanimod (Scott et al, 2016) are effective immunology modulators which are widely used in the treatment of multiple sclerosis.

Fingolimod is being investigated in the management of inflammation caused by COVID-19 (Phase 2 study NCT04280588).
Literature References
PubMed ID Title Journal Year
24900670 Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator

Gao, W, End, P, Pan, S, Mi, Y, Tuntland, T, Heining, P, Gardin, A, Hinterding, K, Fan, Y, Lefebvre, S, Cooke, NG, Chen, Y, Bruns, C, Chu, A, Gray, NS, Nuesslein-Hildesheim, B, Wang, X, Che, J

ACS Med Chem Lett 2013
26990079 Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity

Scott, FL, Rosen, H, Brooks, J, Roberts, E, Martinborough, E, Brahmachary, E, Desale, HG, Timony, GA, Clemons, B, Peach, RJ, Boehm, MF, Dedman, H, Powell, R

Br J Pharmacol 2016
29735753 Metabolism and Disposition of Siponimod, a Novel Selective S1P1/S1P5 Agonist, in Healthy Volunteers and In Vitro Identification of Human Cytochrome P450 Enzymes Involved in Its Oxidative Metabolism

Camenisch, G, Jin, Y, Meissner, A, Nufer, R, Li, W, Legangneux, E, Borell, H, Adam-Stitah, S, Peter van Marle, S, Gardin, A, James, AD, Schroer, K, Glaenzel, U

Drug Metab. Dispos. 2018
20061941 Mechanism of action of oral fingolimod (FTY720) in multiple sclerosis

Hartung, HP, Chun, J

Clin Neuropharmacol 2010
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