De Blasi A, Conn P J, Pin J, Nicoletti F
Institute Mario Negri Sud, St Maria Imbaro, Italy and INM Neuromed, Pozzilli, Italy.
Trends Pharmacol Sci. 2001 Mar;22(3):114-20. doi: 10.1016/s0165-6147(00)01635-7.
Metabotropic glutamate (mglu) receptors are implicated in the regulation of many physiological and pathological processes in the CNS, including synaptic plasticity, learning and memory, motor coordination, pain transmission and neurodegeneration. Several recent studies have elucidated the molecular determinants of mglu receptor signaling and show that several mechanisms acting at different steps in signal propagation are involved. We attempt to offer an integrated view on how homologous and heterologous mechanisms regulate the initial steps of signal propagation, mainly at the level of mglu-receptor-G-protein coupling. Particular emphasis is placed on the role of phosphorylation mechanisms mediated by protein kinase C and G-protein-coupled receptor kinases, and on the emerging importance of some members of the regulators of G-protein signaling family, such as RGS2 and RGS4, which facilitate the GTPase activity that is intrinsic to the alpha-subunits of G(q) and G(i).
代谢型谷氨酸（mglu）受体参与中枢神经系统中许多生理和病理过程的调节，包括突触可塑性、学习与记忆、运动协调、疼痛传递和神经退行性变。最近的几项研究阐明了mglu受体信号传导的分子决定因素，并表明在信号传播的不同步骤中涉及几种作用机制。我们试图提供一个关于同源和异源机制如何调节信号传播初始步骤的综合观点，主要是在mglu受体-G蛋白偶联水平上。特别强调蛋白激酶C和G蛋白偶联受体激酶介导的磷酸化机制的作用，以及G蛋白信号调节家族某些成员（如RGS2和RGS4）的新出现的重要性，它们促进G（q）和G（i）的α亚基固有的GTPase活性。
