摘要
35年以来,对多巴胺(DA)及其受体,尤其是D2受体亚型的研究是一个吸引人且快速发展的科学领域。药物化学、分子和结构生物学以及计算化学的方法被用于DA受体(DR)的研究。描述DR的早期尝试立足于少量可用的实验数据且至多只建立了粗糙的模型。后来我们获得了细菌视紫红质、rhodopsine、多种G蛋白相连的受体和最后的D3 DR受体的晶体结构,并出现了更好更详细的D2 DR受体模型。这些模型使我们了解了配体-受体相互作用的机制,且为新型多巴胺能化合物的合成奠定了基础。其激动剂和拮抗剂可用于治疗各种多巴胺系统不平衡。这篇综述涵盖了D2 DR受体模型创造的道路上关键的发现。
关键词: 3D结构,计算化学,多巴胺,GPCR,同源建模,受体。
Current Medicinal Chemistry
Title:Modeling of Dopamine D2 Receptor - Overview of 35-Year Evolution
Volume: 22 Issue: 25
Author(s): Vladimir Sukalovic, Vukic Soskic and Sladjana Kostic-Rajacic
Affiliation:
关键词: 3D结构,计算化学,多巴胺,GPCR,同源建模,受体。
摘要: Research on dopamine (DA) and its receptors, and in particular the D2 receptor subclass, has been an intriguing and fast developing scientific field in the past 35 years. Methods of medicinal chemistry, molecular and structural biology as well as computational chemistry were used in the studies of DA receptors (DRs). Early attempts to describe DRs were based on a small amount of experimental data available and produced crude models at best. Once crystal structures of bacteriorhodopsin, rhodopsine, various G-protein coupled receptors, and finally D3 DR receptor became available, better and more detailed D2 DR receptor models emerged. These models gave us an insight into the mechanism of ligand-receptor interactions, and paved the way for the synthesis of new dopaminergic compounds, both agonists and antagonists and possible drugs for the treatment of different imbalances of the dopaminergic system. This review covers the key discoveries on the path to the creation of the D2 DR receptor model.
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Vladimir Sukalovic, Vukic Soskic and Sladjana Kostic-Rajacic , Modeling of Dopamine D2 Receptor - Overview of 35-Year Evolution, Current Medicinal Chemistry 2015; 22 (25) . https://dx.doi.org/10.2174/0929867322666150716114316
DOI https://dx.doi.org/10.2174/0929867322666150716114316 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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