Prostaglandin E2 receptor explained

The prostaglandin E₂ (PGE₂) receptors are G protein-coupled receptors that bind and are activated by prostaglandin E₂. They are members of the prostaglandin receptors class of receptors and include the following Protein isoforms:

• Prostaglandin E₂ receptor 1 (EP₁) -
• Prostaglandin E₂ receptor 2 (EP₂) -
• Prostaglandin E₂ receptor 3 (EP₃) -
• Prostaglandin E₂ receptor 4 (EP₄) -

Studies

An antagonist of a prostaglandin E2 receptor has been shown to serve as an affective contraceptive for female macaques while unaffecting their menstrual cyclicity as well as hormonal patterns. The exact reason behind the reduced amount of successful pregnancies of primates during the study is unclear due a number of possibilities that may affect such result.^[1] Inhibition of the prostaglandin E2 EP₄ receptor has been shown to inhibit tumor growth, angiogenesis, lymphangiogenesis, and metastasis. ^{[2] [3]}

Prostaglandin E2 and its effect on inflammation

Prostaglandins are derived from the parent molecule arachidonic acid. The synthesis of prostaglandins can be blocked by anti-inflammatory drugs such as ibuprofen. Anti-inflammatory drugs block the synthesis of cyclooxygenases which in turn produce prostaglandins.^[4] Prostaglandins (PG) are the result of an enzyme cascade pathway that includes two enzymes cyclooxygenase and PG synthase. Prostaglandin E2 is produced by PGE synthase via the activation of EP1-4 receptors. Prostaglandin E2s (PGEs) are associated with the development of vascular diseases that lead to inflammation in the body. In the human body, PGEs are involved in the control of the vascular smooth muscle, cell migration and the division of a cell into two daughter cells.^[5] The process of producing two daughter cells via cell division is called cell proliferation.

See also

• Prostaglandin receptors
• Prostanoid receptors
• Prostaglandin

Notes and References

1. Peluffo . M.C. . Stanley . J. . Braeuer . N. . Rotgeri . A. . Fritzemeier . K.-H. . Fuhrmann . U. . Buchmann . B. . Adevai . T. . Murphy . M.J. . Zelinski . M.B. . Lindenthal . B. . Hennebold . J.D. . Stouffer . R.L. . A prostaglandin E2 receptor antagonist prevents pregnancies during a preclinical contraceptive trial with female macaques . Human Reproduction . July 2014 . 29 . 7 . 1400–1412 . 10.1093/humrep/deu083. 24781425 . 4059334 .
2. Majumder . Mousumi . Xin . Xiping . Liu . Ling . Girish . Gannareddy V. . Lala . Peeyush K. . Prostaglandin E2 receptor EP4 as the common target on cancer cells and macrophages to abolish angiogenesis, lymphangiogenesis, metastasis, and stem-like cell functions . Cancer Science . September 2014 . 105 . 9 . 1142–1151 . 10.1111/cas.12475. 24981602 . 4462388 .
3. Han . ShouWei . Roman . Jesse . Suppression of prostaglandin E2 receptor subtype EP2 by PPARγ ligands inhibits human lung carcinoma cell growth . Biochemical and Biophysical Research Communications . February 2004 . 314 . 4 . 1093–1099 . 10.1016/j.bbrc.2004.01.007. 14751245 .
4. May 2011 . Prostaglandins and Inflammation . Arteriosclerosis, Thrombosis, and Vascular Biology. 31 . 5 . 986–1000 . 10.1161/ATVBAHA.110.207449 . 21508345 . 3081099 . Ricciotti . Emanuela . Fitzgerald . Garret A. .
5. 22 November 2012 . The role of prostaglandin E2 in human vascular inflammation . Prostaglandins, Leukotrienes and Essential Fatty Acids. 89 . 2–3 . 55–63 . 10.1016/j.plefa.2013.04.004 . 23756023 . Gomez . I. . Foudi . N. . Longrois . D. . Norel . X. .