EP4 receptor

EP4 receptor is a protein that in humans is encoded by the PTGER4 gene. It is one of the four prostaglandin E2 (PGE2) receptors, belonging to the G protein-coupled receptor (GPCR) family. The EP4 receptor plays a significant role in various physiological and pathological processes, including inflammation, cancer, and cardiovascular diseases.

Function[edit | edit source]

The EP4 receptor mediates the biological effects of prostaglandin E2, one of the most versatile and potent lipid compounds with wide-ranging effects in the body. Activation of the EP4 receptor by PGE2 leads to a variety of cellular responses, including vasodilation, inhibition of gastric acid secretion, and modulation of immune system responses. In the immune system, the EP4 receptor has been shown to play a role in suppressing inflammation and promoting the resolution phase of the inflammatory response.

Clinical Significance[edit | edit source]

The EP4 receptor has been implicated in the pathogenesis of several diseases. In cancer, EP4 receptor signaling can promote tumor growth, angiogenesis, and metastasis. Consequently, the receptor is considered a potential target for cancer therapy. In the context of inflammatory diseases, such as rheumatoid arthritis and colitis, EP4 receptor antagonists are being explored as therapeutic agents due to their potential to reduce inflammation and tissue damage.

In cardiovascular diseases, the EP4 receptor has a protective role in maintaining cardiovascular homeostasis and promoting angiogenesis following tissue injury. However, the precise role of EP4 receptor signaling in cardiovascular diseases remains complex and is the subject of ongoing research.

Pharmacology[edit | edit source]

Selective EP4 receptor agonists and antagonists have been developed for research and therapeutic purposes. Agonists of the EP4 receptor can mimic the effects of PGE2 and are investigated for their potential to promote tissue repair and regeneration. On the other hand, EP4 receptor antagonists are explored for their ability to inhibit the progression of inflammatory and cancerous diseases.

Genetics[edit | edit source]

The PTGER4 gene encoding the EP4 receptor is located on chromosome 5 in humans. Variations in this gene have been associated with susceptibility to various diseases, including osteoarthritis and inflammatory bowel disease (IBD), highlighting the importance of EP4 receptor signaling in health and disease.