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前列腺素E₂受体亚型1 (EP1)研究进展

陈书涛¹, 季爽², 郭美娜², 陈丽红^2,*

¹大连医科大学基础医学院，大连 116044；²大连医科大学医学科学研究院，大连 116044

摘要

前列腺素E2 (prostaglandin E2, PGE2)是花生四烯酸代谢产生的重要脂质分子，在多种生理和病理活动中发挥重要作用。非甾体抗炎药(non-steroidal anti-inflammatory drugs, NSAIDs)主要通过抑制PGE2的生成而被广泛用于各类炎症性疾病的治疗和发热、疼痛症状的缓解。PGE2功能的发挥主要依赖于与4种不同的G蛋白耦联受体相结合，其中PGE2受体亚型1 (PGE2 receptor 1, EP1)的分布相对比较局限，且PGE2与EP1的亲和力相对较低。尽管如此，EP1在心血管、泌尿、消化等系统的生理功能维持和稳态调节方面却发挥重要作用。此外，EP1广泛参与炎症反应、痛觉维持和多系统的病理生理学功能调节。本文拟就近年来有关EP1在生理和病理生理学方面的功能和研究现状，以及与之相关药物的研究进展进行简要综述。

关键词： 前列腺素E2; 前列腺素E2受体亚型1; 炎症

Research advances of prostaglandin E₂ receptor 1 (EP1)

CHEN Shu-Tao¹, JI Shuang², GUO Mei-Na², CHEN Li-Hong^2,*

¹College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China；²Advanced Institute for Medical Sciences, Dalian Medical University, Dalian 116044, China

Abstract

Prostaglandin E2 (PGE2) is an important lipid molecule derived from arachidonic acid, which regulates a variety of physiological and pathological activities. Based on the inhibition of inflammatory PGE2 production, non-steroidal anti-inflammatory drugs (NSAIDs) are considered as the most commonly used drugs to treat inflammatory diseases and to relieve fever and pain symptoms. PGE2 mediates its functions via four different G protein-coupled receptors, named EP1–EP4. Though the limited distribution and low PGE2 affinity of EP1, it plays important roles in the maintenance of many physiological functions and homeostasis. Moreover, EP1 is widely involved in the inflammatory response, pain perception and multisystem pathological function regulation. In this review, we will briefly summarize the recent advances on the physiological and pathophysiological function of EP1 and its targeted drugs development.

Key words: prostaglandin E2; EP1; inflammation

收稿日期：　　录用日期：

通讯作者：陈丽红　　E-mail: lihong@dmu.edu.cn

DOI: 10.13294/j.aps.2024.0007

引用本文：

陈书涛, 季爽, 郭美娜, 陈丽红. 前列腺素E₂受体亚型1 (EP1)研究进展[J]. 生理学报 2024; 76 (1): 105-118.

CHEN Shu-Tao, JI Shuang, GUO Mei-Na, CHEN Li-Hong. Research advances of prostaglandin E₂ receptor 1 (EP1). Acta Physiol Sin 2024; 76 (1): 105-118 (in Chinese with English abstract).