Biotechnology Institute Thurgau (BITg) at the University of Konstanz, Unterseestrasse 47, Kreuzlingen, Switzerland.
Int J Biochem Cell Biol. 2010 Feb;42(2):198-201. doi: 10.1016/j.biocel.2009.09.015. Epub 2009 Sep 27.
Prostaglandin E(2) (PGE(2)) is the most abundant eicosanoid and a very potent lipid mediator. PGE(2) is produced predominantly from arachidonic acid by its tightly regulated cyclooxygenases (COX) and prostaglandin E synthases (PGES). Secreted PGE(2) acts in an autocrine or paracrine manner through its four cognate G protein coupled receptors EP1 to EP4. Under physiological conditions, PGE(2) is key in many biological functions, such as regulation of immune responses, blood pressure, gastrointestinal integrity, and fertility. Deregulated PGE(2) synthesis or degradation is associated with severe pathological conditions like chronic inflammation, Alzheimer's disease, or tumorigenesis. Therefore, pharmacological inhibition of COX enzymes and PGE(2) receptor antagonism is of great therapeutic interest.
前列腺素 E(2)(PGE(2))是最丰富的类二十烷酸和一种非常有效的脂质介质。PGE(2)主要由其受严密调控的环氧化酶(COX)和前列腺素 E 合酶(PGES)从花生四烯酸产生。分泌的 PGE(2)通过其四个同源 G 蛋白偶联受体 EP1 到 EP4 以自分泌或旁分泌的方式发挥作用。在生理条件下,PGE(2)在许多生物学功能中起关键作用,例如调节免疫反应、血压、胃肠道完整性和生育能力。PGE(2)合成或降解的失调与严重的病理状况有关,如慢性炎症、阿尔茨海默病或肿瘤发生。因此,COX 酶的药理学抑制和 PGE(2)受体拮抗作用具有重要的治疗意义。