摘要
腺苷A2A受体是G-蛋白偶联受体超级家族中的一员。通过中枢神经系统和外周组织,腺苷A2A受体在许多生理过程中起关键作用。在作为拮抗剂用于抗帕金森病药物时,A2A和多巴胺D2受体之间功能性的相互作用激起了研究的兴趣。此外,目前肿瘤药物的设计是基于A2A受体拮抗剂作为免疫治疗的潜力。早期研究是基于第二代药物的经典黄嘌呤类A2A受体拮抗剂,这篇简短的综述涵盖这一类重要药物的研究、开发、化学合成和药物评价的各个方面。
关键词: A2AR拮抗剂、水溶解性、癌症免疫疗法、分子模型、 帕金森氏病、PET成像、 X-射线晶体学
Current Medicinal Chemistry
Title:Towards Next Generation Adenosine A2A Receptor Antagonists
Volume: 21 Issue: 34
Author(s): G. Yuan and G.B. Jones
Affiliation:
关键词: A2AR拮抗剂、水溶解性、癌症免疫疗法、分子模型、 帕金森氏病、PET成像、 X-射线晶体学
摘要: The Adenosine A2A receptor is a member of the G-protein coupled receptor superfamily. It plays a key role in numerous physiological processes through the central nervous system and in peripheral tissues. Functional interactions between the A2A and dopamine D2 receptor has spurred interest in the use of antagonists as anti-Parkinson drugs. Additionally, oncology drugs are now being designed based on the potential for A2A antagonists to function as immunotherapeutics. From early studies based on classical xanthine type A2A antagonists through second generation agents, this mini review will cover aspects of the discovery, development, chemical synthesis and medicinal evaluation of this important class of drugs.
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Cite this article as:
Yuan G. and Jones G.B., Towards Next Generation Adenosine A2A Receptor Antagonists, Current Medicinal Chemistry 2014; 21 (34) . https://dx.doi.org/10.2174/0929867321666140826115123
DOI https://dx.doi.org/10.2174/0929867321666140826115123 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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