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Pharmacology of Adenosine Receptors: The State of the Art.
Physiological Reviews ( IF 29.9 ) Pub Date : 2018-06-01 , DOI: 10.1152/physrev.00049.2017
Pier Andrea Borea 1 , Stefania Gessi 1 , Stefania Merighi 1 , Fabrizio Vincenzi 1 , Katia Varani 1
Affiliation  

Adenosine is a ubiquitous endogenous autacoid whose effects are triggered through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Due to the rapid generation of adenosine from cellular metabolism, and the widespread distribution of its receptor subtypes in almost all organs and tissues, this nucleoside induces a multitude of physiopathological effects, regulating central nervous, cardiovascular, peripheral, and immune systems. It is becoming clear that the expression patterns of adenosine receptors vary among cell types, lending weight to the idea that they may be both markers of pathologies and useful targets for novel drugs. This review offers an overview of current knowledge on adenosine receptors, including their characteristic structural features, molecular interactions and cellular functions, as well as their essential roles in pain, cancer, and neurodegenerative, inflammatory, and autoimmune diseases. Finally, we highlight the latest findings on molecules capable of targeting adenosine receptors and report which stage of drug development they have reached.

中文翻译:

腺苷受体的药理学:最新技术。

腺苷是一种普遍存在的内源性autaucoid,其作用是通过四个G蛋白偶联受体:A1,A2A,A2B和A3的参与而触发的。由于腺苷从细胞代谢中快速生成,并且其受体亚型在几乎所有器官和组织中广泛分布,因此该核苷可诱导多种生理病理作用,调节中枢神经,心血管,外周和免疫系统。逐渐清楚的是,腺苷受体的表达模式在细胞类型之间有所不同,这使人们认为腺苷受体可能既是病理学的标志,又是新药的有用靶标。这篇综述概述了腺苷受体的最新知识,包括其特征性结构特征,分子相互作用和细胞功能,以及它们在疼痛,癌症以及神经退行性,炎性和自身免疫性疾病中的重要作用。最后,我们重点介绍了能够靶向腺苷受体的分子的最新发现,并报告了它们已进入药物开发的哪个阶段。
更新日期:2019-11-01
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