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目前作为潜在治疗药物的腺苷 A3 受体激动剂和拮抗剂的设计和开发现状。

Current Status in the Design and Development of Agonists and Antagonists of Adenosine A3 Receptor as Potential Therapeutic Agents.

机构信息

Department of Pharmaceutical Chemistry, Shri Vishnu College of Pharmacy, Vishnupur (Affiliated to Andhra University), Bhimavaram, W.G. Dist., AP, India.

Faculty of Pharmacy, Philadelphia University-Jordan, P.O BOX (1), Philadelphia University- 19392, Amman, Jordan.

出版信息

Curr Pharm Des. 2019;25(25):2772-2787. doi: 10.2174/1381612825666190716114056.

DOI:10.2174/1381612825666190716114056
PMID:31333098
Abstract

Adenosine receptors (ARs) belongs to the family of G-protein coupled receptors (GPCR) that are responsible for the modulation of a wide variety of physiological functions. The ARs are also implicated in many diseases such as cancer, arthritis, cardiovascular and renal diseases. The adenosine A3 receptor (A3AR) has emerged as a potential drug target for the progress of new and effective therapeutic agents for the treatment of various pathological conditions. This receptor's involvement in many diseases and its validity as a target has been established by many studies. Both agonists and antagonists of A3AR have been extensively investigated in the last decade with the goal of developing novel drugs for treating diseases related to immune disorders, inflammation, cancer, and others. In this review, we shall focus on the medicinal chemistry of A3AR ligands, exploring the diverse chemical classes that have been projected as future leading drug candidates. Also, the recent advances in the therapeuetic applications of A3AR ligands are highlighted.

摘要

腺苷受体(ARs)属于 G 蛋白偶联受体(GPCR)家族,负责调节多种生理功能。ARs 也与许多疾病有关,如癌症、关节炎、心血管和肾脏疾病。腺苷 A3 受体(A3AR)已成为开发用于治疗各种病理状况的新型有效治疗剂的潜在药物靶点。该受体在许多疾病中的作用及其作为靶点的有效性已被许多研究证实。在过去十年中,A3AR 的激动剂和拮抗剂都得到了广泛的研究,目的是开发用于治疗与免疫紊乱、炎症、癌症等相关疾病的新型药物。在这篇综述中,我们将重点介绍 A3AR 配体的药物化学,探索已被预测为未来主要候选药物的各种化学类别。此外,还强调了 A3AR 配体在治疗应用方面的最新进展。

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