| 陈京,姜云璐.GPCRs二聚体:功能和药理作用展望[J].济宁医学院学报,2015,(1):1-7,25 |
| GPCRs二聚体:功能和药理作用展望 |
| G protein coupled receptors oligomerization:functional and pharmacological perspectives |
| 投稿时间：2015-03-10 |
| DOI：10.3969/j.issn.1000-9760.2015.01.001 |
| 中文关键词: G蛋白偶联受体 变构调节 荧光相关光谱 全内反射显微镜 |
| 英文关键词: G protein-coupled receptor Allosteric regulation Fluorescence correlation spectroscopy Total internal reflection fluorescence microscope |
| 基金项目:国家自然科学基金项目(编号:3097108,31271243,81070961)山东省自然科学基金项目(编号:ZR2011CM027,2012GSF11806) |
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| 中文摘要: |
| G蛋白偶联受体是最大的膜受体超家族之一,参与调节多种生理过程,在信号识别及转导中具有重要作用,是医学研究与计划的焦点之一,但基于GPCRs单体的药物通常疗效欠佳、副作用较多。随着GPCRs二聚体的不断证实,二聚体不同于单体的内在疗效、配体选择及由变构调节引起的功能选择性,在临床疾病治疗及新药研发中倍受关注。本文基于检测GPCRs二聚体的技术,就GPCRs二聚体形成的决定因素、功能及药理学作用作一综述。 |
| 英文摘要: |
| G protein-coupled receptors (GPCRs),one of the largest membrane receptor superfamily,which can regulate a variety of downstream signaling pathways,is one of the central issues of medical research and program.The drugs based on monomeric GPCRs usually accompany with side effects.But with the proven of GPCRs dimers and oligomers,oligomers has been gazed in clinical disease treatment and drug development because of the differences with monomer in intrinsic efficacy,ligand choice and functional selectivity which is induced by allosteric regulation.In this article,the determinants of conformation,function and pharmacological effect of GPCRs oligomers are discussed comprehensive. |
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