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International Union of Basic and Clinical Pharmacology. CIX. Differences and Similarities between Human and Rodent Prostaglandin E2 Receptors (EP1-4) and Prostacyclin Receptor (IP): Specific Roles in Pathophysiologic Conditions.
Pharmacological Reviews ( IF 19.3 ) Pub Date : 2020-10-01 , DOI: 10.1124/pr.120.019331
Xavier Norel 1 , Yukihiko Sugimoto 2 , Gulsev Ozen 2 , Heba Abdelazeem 2 , Yasmine Amgoud 2 , Amel Bouhadoun 2 , Wesam Bassiouni 2 , Marie Goepp 2 , Salma Mani 2 , Hasanga D Manikpurage 2 , Amira Senbel 2 , Dan Longrois 2 , Akos Heinemann 2 , Chengcan Yao 2 , Lucie H Clapp 2
Affiliation  

Prostaglandins are derived from arachidonic acid metabolism through cyclooxygenase activities. Among prostaglandins (PGs), prostacyclin (PGI2) and PGE2 are strongly involved in the regulation of homeostasis and main physiologic functions. In addition, the synthesis of these two prostaglandins is significantly increased during inflammation. PGI2 and PGE2 exert their biologic actions by binding to their respective receptors, namely prostacyclin receptor (IP) and prostaglandin E2 receptor (EP) 1–4, which belong to the family of G-protein–coupled receptors. IP and EP1–4 receptors are widely distributed in the body and thus play various physiologic and pathophysiologic roles. In this review, we discuss the recent advances in studies using pharmacological approaches, genetically modified animals, and genome-wide association studies regarding the roles of IP and EP1–4 receptors in the immune, cardiovascular, nervous, gastrointestinal, respiratory, genitourinary, and musculoskeletal systems. In particular, we highlight similarities and differences between human and rodents in terms of the specific roles of IP and EP1–4 receptors and their downstream signaling pathways, functions, and activities for each biologic system. We also highlight the potential novel therapeutic benefit of targeting IP and EP1–4 receptors in several diseases based on the scientific advances, animal models, and human studies.

中文翻译:


国际基础与临床药理学联盟。 CIX。人类和啮齿动物前列腺素 E2 受体 (EP1-4) 和前列环素受体 (IP) 之间的差异和相似之处:在病理生理状况中的特定作用。



前列腺素源自花生四烯酸通过环氧合酶活性的代谢。在前列腺素(PG)中,前列环素(PGI 2 )和PGE 2强烈参与体内平衡和主要生理功能的调节。此外,这两种前列腺素的合成在炎症期间显着增加。 PGI 2和PGE 2通过与其各自的受体结合来发挥其生物学作用,即前列环素受体(IP) 和前列腺素E 2受体(EP) 1-4,它们属于G 蛋白偶联受体家族。 IP和EP1-4受体广泛分布于体内,发挥着多种生理和病理生理作用。在这篇综述中,我们讨论了使用药理学方法、转基因动物和全基因组关联研究的最新进展,这些研究涉及 IP 和 EP1-4 受体在免疫、心血管、神经、胃肠道、呼吸系统、泌尿生殖系统和神经系统中的作用。肌肉骨骼系统。我们特别强调了人类和啮齿动物在 IP 和 EP1-4 受体的具体作用及其下游信号通路、功能和每个生物系统活动方面的相似之处和差异。我们还根据科学进展、动物模型和人体研究,强调了针对 IP 和 EP1-4 受体在多种疾病中的潜在新治疗益处。
更新日期:2020-09-22
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