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Sphingosine 1-phosphate receptor modulators (S1PR modulators) are a class of drugs that target sphingosine 1-phosphate receptors (S1PRs), which are G protein-coupled receptors involved in regulating immune cell trafficking, vascular integrity, and other physiological processes. These drugs have become important in the treatment of autoimmune diseases, especially multiple sclerosis (MS), due to their ability to modulate lymphocyte movement and reduce neuroinflammation. The main mechanism by which these modulators exert their effect is by binding to the receptor on lymphocytes, effectively antagonizing it, limiting lymphocyte egress from lymph nodes.
Functional antagonism via ligand-induced internalization; blocks egress of immune cells from lymph nodes, reducing circulating lymphocytes.
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