Chen Shu-Tao, Ji Shuang, Guo Mei-Na, Chen Li-Hong
College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China.
Advanced Institute for Medical Sciences, Dalian Medical University, Dalian 116044, China.
Sheng Li Xue Bao. 2024 Feb 25;76(1):105-118.
Prostaglandin E (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 PGE 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. PGE mediates its functions via four different G protein-coupled receptors, named EP1-EP4. Though the limited distribution and low PGE 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.
前列腺素E(PGE2)是一种源自花生四烯酸的重要脂质分子,它调节多种生理和病理活动。基于对炎性PGE产生的抑制作用,非甾体抗炎药(NSAIDs)被认为是治疗炎性疾病以及缓解发热和疼痛症状最常用的药物。PGE通过四种不同的G蛋白偶联受体(称为EP1-EP4)介导其功能。尽管EP1分布有限且对PGE的亲和力较低,但它在维持许多生理功能和体内平衡中发挥着重要作用。此外,EP1广泛参与炎症反应、疼痛感知和多系统病理功能调节。在本综述中,我们将简要总结EP1的生理和病理生理功能及其靶向药物开发的最新进展。