Progress in research of constitutive activity of G protein-coupled receptors and their role in new drug discovery
文献类型：期刊论文
| 作者 | Hong Minhua; Chi Zhiqiang ; Liu Jinggen
|
| 刊名 | Chinese Pharmacological Bulletin
 |
| 出版日期 | 2005 |
| 卷号 | 21期号:9页码:1030-1033 |
| 关键词 | G-protein-coupled receptors ( GPCR ) constitutive activity |
| ISSN号 | 1001-1978 |
| 其他题名 | G蛋白偶联受体固有活性研究进展与新药开发 |
| 文献子类 | Review |
| 英文摘要 | G-prolein-coupled receptos ((?PCRs) are the largest superfamily of cell surface receptors, which couple G-proteins. The structures of GPCRs contain seven transmembrane domians. The unique structure and important role in the signaling transduction of GPCRs make them act as very useful drug targets. The GPCRs have great pharmacological importance and their agonists or antagonists have great potential to be?come the new drugs agnist diseases. So far, one third of approved small molecular drugs sold in market are the agonists or antaginists of GPCRs. Among the 50 kinds of most popular drugs approved recently, 20% of them belonged to GPCR. Recent studies demonstrate that GPCR has a very important feature; constitutive activity, which can described as the ability of a GPCR to undergo agonist-independent isomerization by which it can spontaneouly stimulates and maintains down?stream signal transduclion. Constitutive activity in?volves interaction of receptors, G proteins, and down?stream signal transduction pathways. The present re?view elaborated the concept of constitutive activity, in?verse agonist and progress in research of constitutive ac?tivity of G protein-coupled receptors and their role in new drug discovery. |
| 资助项目 | 中国科学院"百人计划"研究基金[00000000] ; 国家杰出青年科学基金资助项目[00000000] ; 国家重点基础研究发展计划资助项目[00000000] |
| WOS研究方向 | General & Internal Medicine (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:2152126 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/268311]  |
| 专题 | 药理学第二研究室 |
| 通讯作者 | Liu Jinggen |
| 作者单位 | State key laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China. |
| 推荐引用方式 GB/T 7714 | Hong Minhua,Chi Zhiqiang,Liu Jinggen. Progress in research of constitutive activity of G protein-coupled receptors and their role in new drug discovery[J]. Chinese Pharmacological Bulletin,2005,21(9):1030-1033. |
| APA | Hong Minhua,Chi Zhiqiang,&Liu Jinggen.(2005).Progress in research of constitutive activity of G protein-coupled receptors and their role in new drug discovery.Chinese Pharmacological Bulletin,21(9),1030-1033. |
| MLA | Hong Minhua,et al."Progress in research of constitutive activity of G protein-coupled receptors and their role in new drug discovery".Chinese Pharmacological Bulletin 21.9(2005):1030-1033. |
入库方式： OAI收割
来源：上海药物研究所
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