S1PR3

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S1PR3

The S1PR3, also known as the Sphingosine-1-phosphate receptor 3, is a G protein-coupled receptor that plays a crucial role in various physiological processes. It is a member of the S1P receptor family and is primarily expressed in the cardiovascular and immune systems.

Structure

The S1PR3 receptor is encoded by the S1PR3 gene located on chromosome 12q13.13 in humans. It consists of 7 transmembrane domains and an extracellular N-terminus. The intracellular C-terminus is responsible for coupling with G proteins, which initiates downstream signaling pathways upon ligand binding.

Function

The S1PR3 receptor is activated by the lipid signaling molecule sphingosine-1-phosphate (S1P). Upon binding of S1P, the receptor undergoes conformational changes, leading to the activation of G proteins. This activation triggers a cascade of intracellular signaling events, including the activation of various kinases and the modulation of ion channels.

The S1PR3 receptor is involved in the regulation of vascular tone, immune cell trafficking, and lymphocyte development. In the cardiovascular system, activation of S1PR3 leads to vasodilation and the inhibition of smooth muscle cell proliferation. In the immune system, it plays a role in the migration of immune cells, such as lymphocytes, to lymphoid organs and inflammatory sites.

Clinical Significance

Due to its involvement in various physiological processes, dysregulation of the S1PR3 receptor has been implicated in several diseases. For example, aberrant S1PR3 signaling has been associated with cardiovascular diseases, including hypertension and atherosclerosis. In addition, it has been linked to autoimmune diseases, such as multiple sclerosis and rheumatoid arthritis, due to its role in immune cell trafficking.

Pharmaceutical companies have recognized the therapeutic potential of targeting the S1PR3 receptor. Selective modulators of S1PR3 are being developed as potential treatments for cardiovascular diseases and autoimmune disorders. These modulators aim to either activate or inhibit the receptor, depending on the specific disease and desired therapeutic outcome.

References

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