Faculty of Pharmacy, Philadelphia University-Jordan, P.O BOX (1), Philadelphia University-19392, Amman, Jordan.
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
Curr Pharm Des. 2019;25(25):2716-2740. doi: 10.2174/1381612825666190716113444.
Adenosine receptors (ARs) are a class of G-protein coupled receptors (GPCRs) that are activated by the endogenous substance adenosine. ARs are classified into 4 subtype receptors, namely, the A1, A2A, A2B and A3 receptors. The wide distribution and expression of the ARs in various body tissues as well as the roles they have in controlling different functions in the body make them potential drug targets for the treatment of various pathological conditions, such as cardiac diseases, cancer, Parkinson's disease, inflammation and glaucoma. Therefore, in the past decades, there have been extensive investigations of ARs with a high number of agonists and antagonists identified that can interact with these receptors. This review shall discuss the A2A receptor (A2AAR) subtype of the ARs. The structure, properties and the recent advances in the therapeutic potential of the receptor are discussed with an overview of the recent advances in the methods of studying the receptor. Also, molecular modeling approaches utilized in the design of A2AAR ligands are highlighted with various recent examples.
腺苷受体（ARs）是一类 G 蛋白偶联受体（GPCRs），它们被内源性物质腺苷激活。ARs 分为 4 种亚型受体，即 A1、A2A、A2B 和 A3 受体。ARs 在各种身体组织中的广泛分布和表达，以及它们在控制身体不同功能方面的作用，使它们成为治疗各种病理状况（如心脏病、癌症、帕金森病、炎症和青光眼）的潜在药物靶点。因此，在过去几十年中，人们对 ARs 进行了广泛的研究，发现了大量可以与这些受体相互作用的激动剂和拮抗剂。本综述将讨论 ARs 的 A2A 受体（A2AAR）亚型。讨论了受体的结构、特性和治疗潜力的最新进展，并概述了研究受体的方法的最新进展。此外，还强调了在设计 A2AAR 配体中使用的分子建模方法，并列举了各种最新实例。
