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G-Protein Coupled Receptors Involved in the Resolution of Inflammation: Ligands and Therapeutic Perspectives
Mini-Reviews in Medicinal Chemistry ( IF 3.8 ) Pub Date : 2020-11-30 , DOI: 10.2174/1389557520666200719014433
Margherita Mastromarino 1 , Enza Lacivita 1 , Nicola A. Colabufo 1 , Marcello Leopoldo 1
Affiliation  

Dysregulated inflammation is a central pathological process in diverse disease states, including neurodegenerative disorders. The recent concept of “resolution of inflammation” is offering a conceptual change for the diagnosis and the development of new therapeutic approaches for chronic inflammatory diseases. Resolution of inflammation terminates the inflammatory response promoting the return to tissue homeostasis through the action of several classes of mediators, termed specialized pro-resolving lipid mediators (SPMs), that include lipoxins, resolvins, protectins, and maresins. SPMs provide “stop signals” that reduce the number of immune cells at the site of insult and increase the clearance of apoptotic cells through phagocytosis. SPMs elicit their effects through the interaction with specific G-protein coupled receptors (GPCRs). The elucidation of the pathways downstream of the GPCRs involved in the resolution of chronic inflammation is opening novel opportunities to generate novel anti-inflammatory agents. This review focuses on the SPMs and the receptors through which their effects are mediated. The medicinal chemistry of the modulators of the GPCRs involved in the resolution of inflammation will be illustrated, by highlighting the potential for developing new antiinflammatory drugs.



中文翻译:

G蛋白偶联受体参与炎症的解决:配体和治疗的观点。

炎症失调是包括神经退行性疾病在内的多种疾病状态的主要病理过程。最近的“炎症消退”概念为诊断和开发慢性炎性疾病的新治疗方法提供了观念上的变化。炎症的消退终止了炎症反应,通过几类介体的作用促进了组织稳态的恢复,这些介体被称为专门的促分解脂质介体(SPM),包括脂蛋白,resolvins,protectin和maresins。SPM可提供“停止信号”,从而减少损伤部位免疫细胞的数量,并通过吞噬作用增加凋亡细胞的清除率。SPM通过与特定的G蛋白偶联受体(GPCR)相互作用引发其作用。对参与慢性炎症解决的GPCRs下游途径的阐明为产生新型抗炎药打开了新的机会。这篇综述着重于SPM及其介导其作用的受体。通过强调开发新抗炎药的潜力,将说明参与炎症消除的GPCR调节剂的药物化学作用。

更新日期:2021-01-15
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