| G蛋白偶联受体组成性活性及反向激动剂研究进展 |
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| 引用本文： | 孙洪良,郑建全.G蛋白偶联受体组成性活性及反向激动剂研究进展[J].国际药学研究杂志,2007,34(1):39-43. |
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| 作者姓名： | 孙洪良 郑建全 |
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| 作者单位： | 军事医学科学院毒物药物研究所,北京,100850 |
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| 摘 要： | G蛋白偶联受体（GPCR）是受体中家族成员最多的一大类，其活性涉及体内绝大部分的生理功能，在药物研发过程中是主要的药物作用靶标。研究表明，GPCR及其突变体在缺乏配体结合的情况下，能自发地产生一定程度的内在活性，即GPCR的组成性活性（constitutive activity）；其相应的反向激动剂与GPCR结合能降低受体的组成性活性，在药物治疗学上具有重要意义。愈来愈多的实验表明，GPCR组成性活性及反向激动剂的研究具有广阔和实际的应用前景，对其进行深入研究在受体学说领域和药物研发过程中具有重要理论意义。
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| 关 键 词： | G蛋白偶联受体 组成性活性 反向激动剂 |
| 文章编号： | 1001-0971(2007)01-0039-05 |
| 收稿时间： | 2006-5-31 |
| 修稿时间： | 2006年5月31日 |
Advances in research on constitutive activity and inverse agonists of G protein-coupled receptors |
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| SUN Hong-liang,ZHENG Jian-quan.Advances in research on constitutive activity and inverse agonists of G protein-coupled receptors[J].Foreign Medical Sciences(Section of Pharmarcy),2007,34(1):39-43. |
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| Authors: | SUN Hong-liang ZHENG Jian-quan |
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| Affiliation: | (Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China) |
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| Abstract: | G protein coupled receptors (GPCR)belong to a superfamily of receptors and have numerous members The activation of GPCR contributes to the most of physiological functions In recent years, accumulative evidence confirms the occurrence of constitutive activity of GPCR in the absence of agonist stimulation A new concept of inverse agonists is raised and accepted for some compounds. It can inversely activate GPCR by decreasing the constitutive activity The new progress in the research on the constitutive activity and inverse agonists of GPCR displays an important significance in application of the receptor theory, and practical values for drug development. |
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| Keywords: | GPCR constitutive activity inverse agonist |
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