Department of Organic Chemistry, Gdansk University of Technology, G. Narutowicza 11/12, PL 80-952 Gdańsk, Poland.
Pharmacol Rep. 2011;63(3):601-17. doi: 10.1016/s1734-1140(11)70573-4.
This review summarizes current knowledge of adenosine analogues and conjugates with promising therapeutic properties. Adenosine is a signaling molecule that triggers numerous physiological responses. It acts through the adenosine receptors (ARs), belonging to the family of G-protein-coupled receptors and widely distributed throughout the body. Moreover, adenosine is involved in key biochemical processes as a part of ATP, the universal energy currency. Thus, compounds that are analogues of adenosine and its conjugates have been extensively studied as potential therapeutics. Many inhibitors of ARs are in clinical trials as promising agents in treatment of inflammation, type 2 diabetes, arrhythmia and as vasodilators used in the myocardial perfusion imaging (MPI) stress test. Furthermore, adenosine analogues revealed high efficacy as enzyme inhibitors, tested for antitrypanosomal action and as bivalent ligands and adenosine-oligoarginine conjugates as inhibitors of protein kinases.
本文综述了具有潜在治疗特性的腺苷类似物和缀合物的最新知识。腺苷是一种信号分子，可引发多种生理反应。它通过属于 G 蛋白偶联受体家族的腺苷受体 (AR) 发挥作用，广泛分布于全身。此外，作为通用能量货币的 ATP 的一部分，腺苷参与关键的生化过程。因此，作为潜在治疗药物，腺苷及其缀合物的类似物已被广泛研究。许多 AR 抑制剂正在临床试验中作为治疗炎症、2 型糖尿病、心律失常和心肌灌注成像 (MPI) 应激试验中使用的血管扩张剂的有前途的药物。此外，腺苷类似物作为酶抑制剂、抗锥虫作用以及作为二价配体和腺苷-寡精氨酸缀合物的蛋白激酶抑制剂显示出很高的功效。
