Endothelin A receptor

Endothelin A receptor (ET_A receptor) is a type of endothelin receptor that has a high affinity for endothelin-1. It is a G protein-coupled receptor (GPCR) that is primarily found in the vascular smooth muscle where it plays a role in vasoconstriction and cell proliferation.

Structure

The ET_A receptor is a 427-amino acid protein that belongs to the GPCR family. It has seven transmembrane domains, an extracellular N-terminus, and an intracellular C-terminus. The receptor's structure allows it to bind to endothelin-1 and initiate a cascade of intracellular events.

Function

The primary function of the ET_A receptor is to mediate the effects of endothelin-1, a potent vasoconstrictor. When endothelin-1 binds to the ET_A receptor, it activates the G protein, which in turn activates a series of intracellular signaling pathways. These pathways lead to the contraction of vascular smooth muscle cells, resulting in vasoconstriction.

In addition to its role in vasoconstriction, the ET_A receptor also plays a role in cell proliferation. It has been found to be overexpressed in several types of cancer, including ovarian cancer, prostate cancer, and melanoma.

Clinical significance

Due to its role in vasoconstriction and cell proliferation, the ET_A receptor is a potential target for the treatment of various cardiovascular and cancerous diseases. Several ET_A receptor antagonists have been developed and are currently in clinical trials.

See also

• Endothelin receptor
• Endothelin-1
• G protein-coupled receptor
• Vascular smooth muscle

References

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