Soudijn Willem, van Wijngaarden Ineke, Ijzerman Adriaan P
Leiden/Amsterdam Center for Drug Research, PO Box 9502, 2300RA Leiden, The Netherlands.
Med Res Rev. 2005 Jul;25(4):398-426. doi: 10.1002/med.20031.
It has been recently established that G-protein-coupled receptors (GPCRs) can be constitutively active, i.e., they can be active in the absence of an agonist. This activity can be inhibited by so-called inverse agonists. For a number of GPCRs, such inverse agonists have been developed and studied, now enabling for the first time a study into their structure-activity relationships.
最近已经确定，G蛋白偶联受体（GPCRs）可以组成性激活，即它们在没有激动剂的情况下也可以激活。这种活性可以被所谓的反向激动剂抑制。对于许多GPCRs，已经开发并研究了此类反向激动剂，现在首次能够对它们的构效关系进行研究。
