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) inhibitors possess immunomodulatory/immunosuppresant actions. The S1PR1 inhibitors fingolimod (FTY720) (Chun & Hartung 2010) and siponimod (BAF312) (Pan et al. 2013, Glaenzel et al. 2018) 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
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

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

Drug Metab. Dispos. 2018
24900670 Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator

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

ACS Med Chem Lett 2013
20061941 Mechanism of action of oral fingolimod (FTY720) in multiple sclerosis

Chun, J, Hartung, HP

Clin Neuropharmacol 2010
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