A2B 腺苷受体配体的治疗潜力：现状与展望。
Therapeutic Potentials of A2B Adenosine Receptor Ligands: Current Status and Perspectives.
机构信息
Faculty of Pharmacy, Philadelphia University-Jordan, P. O. Box: 1, Philadelphia University-19392, Amman, Jordan.
College of Health Sciences, University of KwaZulu-Natal, P. O. Box: 4000, Westville, Durban, South Africa.
出版信息
Curr Pharm Des. 2019;25(25):2741-2771. doi: 10.2174/1381612825666190717105834.
BACKGROUND
Adenosine receptors (ARs) are classified as A1, A2A, A2B, and A3 subtypes belong to the superfamily of G-protein coupled receptors (GPCRs). More than 40% of modern medicines act through either activation or inhibition of signaling processes associated with GPCRs. In particular, A2B AR signaling pathways are implicated in asthma, inflammation, cancer, ischemic hyperfusion, diabetes mellitus, cardiovascular diseases, gastrointestinal disorders, and kidney disease.
METHODS
This article reviews different disease segments wherein A2B AR is implicated and discusses the potential role of subtype-selective A2B AR ligands in the management of such diseases or disorders. All the relevant publications on this topic are reviewed and presented scientifically.
RESULTS
This review provides an up-to-date highlight of the recent advances in the development of novel and selective A2B AR ligands and their therapeutic role in treating various disease conditions. A special focus has been given to the therapeutic potentials of selective A2B AR ligands in the management of airway inflammatory conditions and cancer.
CONCLUSIONS
This systematic review demonstrates the current status and perspectives of A2B AR ligands as therapeutically useful agents that would assist medicinal chemists and pharmacologists in discovering novel and subtype-selective A2B AR ligands as potential drug candidates.
背景
腺苷受体（AR）分为 A1、A2A、A2B 和 A3 四种亚型，属于 G 蛋白偶联受体（GPCR）超家族。超过 40%的现代药物通过激活或抑制与 GPCR 相关的信号转导过程发挥作用。特别是 A2B AR 信号通路与哮喘、炎症、癌症、缺血性过度灌注、糖尿病、心血管疾病、胃肠道疾病和肾脏疾病有关。
方法
本文综述了 A2B AR 参与的不同疾病领域，并讨论了亚型选择性 A2B AR 配体在这些疾病或病症管理中的潜在作用。综述了该主题的所有相关出版物，并进行了科学呈现。
结果
本文综述提供了新型和选择性 A2B AR 配体的最新进展以及它们在治疗各种疾病方面的治疗作用的最新亮点。特别关注选择性 A2B AR 配体在气道炎症和癌症管理中的治疗潜力。
结论
本文系统评价表明，A2B AR 配体作为治疗有用的药物具有当前的地位和前景，这将有助于药物化学家和药理学家发现新型和亚型选择性 A2B AR 配体作为潜在的药物候选物。
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