G蛋白偶联受体组成性活性及反向激动剂研究进展

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。

Advances in research on constitutive activity and inverse agonists of G protein-coupled receptors

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.