Fuxe Kjell, Marcellino Daniel, Guidolin Diego, Woods Amina S, Agnati Luigi F
Department of Neuroscience, Karolinska Institutet, Stockholm, Sweden.
Physiology (Bethesda). 2008 Dec;23:322-32. doi: 10.1152/physiol.00028.2008.
Through an assembly of interacting GPCRs, heterodimers and high-order heteromers (termed receptor mosaics) are formed and lead to changes in the agonist recognition, signaling, and trafficking of participating receptors via allosteric mechanisms, sometimes involving the appearance of cooperativity. This field has now become a major research area, and this review deals with their physiology being integrators of receptor signaling in the CNS and their use as targets for novel drug development based on their unique pharmacology.
通过相互作用的G蛋白偶联受体(GPCR)组装,形成异二聚体和高阶异聚体(称为受体镶嵌体),并通过变构机制导致参与受体的激动剂识别、信号传导和转运发生变化,有时还涉及协同性的出现。该领域现已成为一个主要的研究领域,本综述探讨了它们作为中枢神经系统中受体信号整合器的生理学特性,以及基于其独特药理学特性作为新型药物开发靶点的应用。