| G蛋白偶联受体二聚化在药物开发中所发挥的特异性作用(英文) |
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| 引用本文： | 蔡欣,陈京,白波.G蛋白偶联受体二聚化在药物开发中所发挥的特异性作用(英文)[J].中国药学,2011,20(6):535-541. |
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| 作者姓名： | 蔡欣 陈京 白波 |
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| 作者单位： | 泰山医学院基础医学部神经生物学;济宁医学院神经生物研究所;英国华威大学华威医学院; |
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| 基金项目： | National Natural Science Foundation of China(Grant No.30971081,30870932,and 81070961); Shandong Provincial Natural Science Foundation(Grant No.Y2007D01 and ZR2009DZ004) |
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| 摘 要： | G蛋白偶联受体(GPCRs)是与G蛋白相偶联的七次跨膜受体,其成员有上千种,是重要的药物靶点之一。目前,GPCRs相关药物占市场上药物的40%-50%。在过去的十年中,对GPCRs主要以单体的形式存在着的这一假说做出了重新评估,大量事实证明GPCRs也能以同源或异源二聚体,甚至是高阶寡聚体的形式存在,比较热门的领域是GPCRs二聚化。最近研究表明同源或异源二聚化有不同于单体的特异功能特征,包括配体识别、信号转导、运输等。同时,在较少副作用治疗疾病的新药开发上,具有不同病理和信号转导途径的二聚体的出现开辟了新的领域。本综述主要介绍二聚体的特异结构及其特异的信号转导途径,从而有助于在GPCRs药物开发中取得丰硕的成果。
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| 关 键 词： | G蛋白偶联受体 二聚化 信号转导 药物开发 |
Exploring the specific role of GPCRs dimerization in drug discovery |
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| Xin Cai,Jing Chen,Bo Bai.Exploring the specific role of GPCRs dimerization in drug discovery[J].Journal of Chinese Pharmaceutical Sciences,2011,20(6):535-541. |
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| Authors: | Xin Cai Jing Chen Bo Bai |
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| Institution: | Xin Cai~1,Jing Chen~(2,3),Bo Bai~(2*) 1.Department of Preclinical Medicine,Taishan Medical University,Tai'an 271000,China 2.Neurobiology Institute,Jining Medical University,Jining 272000,China 3.Warwick Medical School,University of Warwick,England 999020,United Kingdom |
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| Abstract: | G-protein-coupled receptors(GPCRs) are G-protein-coupled heptaspanning-membrane receptors.This group has thousands of members and is one of the important drug targets,accounting for 40%-50%of the drugs currently on the market.In the last decade,there has been a substantial re-evaluation of the assumption that GPCRs exist primarily as monomeric polypeptides, with support increasing for a model in which GPCRs can exist as homo- or hetero- dimers or even high-order oligomers.GPCRs dimers are hot research topic... |
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| Keywords: | G-protein-coupled receptors Receptor dimers Signal transduction Drug discovery |
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