腺苷受体作为治疗靶点。
Adenosine receptors as therapeutic targets.
作者信息
Jacobson Kenneth A, Gao Zhan-Guo
机构信息
Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0810, USA.
出版信息
Nat Rev Drug Discov. 2006 Mar;5(3):247-64. doi: 10.1038/nrd1983.
Abstract
Adenosine receptors are major targets of caffeine, the most commonly consumed drug in the world. There is growing evidence that they could also be promising therapeutic targets in a wide range of conditions, including cerebral and cardiac ischaemic diseases, sleep disorders, immune and inflammatory disorders and cancer. After more than three decades of medicinal chemistry research, a considerable number of selective agonists and antagonists of adenosine receptors have been discovered, and some have been clinically evaluated, although none has yet received regulatory approval. However, recent advances in the understanding of the roles of the various adenosine receptor subtypes, and in the development of selective and potent ligands, as discussed in this review, have brought the goal of therapeutic application of adenosine receptor modulators considerably closer.
摘要
腺苷受体是咖啡因的主要作用靶点，咖啡因是世界上消费最为广泛的药物。越来越多的证据表明，在包括脑和心脏缺血性疾病、睡眠障碍、免疫和炎症性疾病以及癌症在内的多种病症中，腺苷受体也可能是很有前景的治疗靶点。经过三十多年的药物化学研究，已经发现了相当数量的腺苷受体选择性激动剂和拮抗剂，其中一些已经进行了临床评估，尽管尚未有任何一种获得监管部门的批准。然而，如本综述中所讨论的，在对各种腺苷受体亚型作用的理解以及选择性强效配体的开发方面取得的最新进展，已使腺苷受体调节剂的治疗应用目标更近了一步。
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