Brennan Sarah C, Conigrave Arthur D
School of Molecular and Microbial Biosciences, University of Sydney, NSW 2006, Australia.
Curr Pharm Biotechnol. 2009 Apr;10(3):270-81. doi: 10.2174/138920109787847484.
The extracellular calcium-sensing receptor (CaR) is a class III G-protein coupled receptor that coordinates cellular responses to changes in extracellular free Ca(2+) or amino acid concentrations as well as ionic strength and pH. It regulates signalling cascades via recruiting and controlling the activities of various heterotrimeric G-proteins, including G(q/11), G(i/0), and G(12/13), even G(s) in some "unusual" circumstances, thereby inducing changes in the metabolism of membrane lipids, the phosphorylation state of protein kinases and their targets, the activation state of monomeric G-proteins and the levels of intracellular second messengers including cAMP, Ca(2+) ions, fatty acids and other small molecules. According to its site(s) of expression and available signalling pathways, the CaR modulates cell proliferation and survival, differentiation, peptide hormone secretion, ion and water transport and various other processes. In this article we consider the complex intracellular mechanisms by which the CaR elicits its cellular functions. We also consider some of the better understood CaR-regulated cell functions and the nature of the signalling mechanisms that support them.
细胞外钙敏感受体(CaR)是一种III类G蛋白偶联受体,可协调细胞对细胞外游离Ca(2+)、氨基酸浓度以及离子强度和pH值变化的反应。它通过招募和控制各种异源三聚体G蛋白(包括G(q/11)、G(i/0)和G(12/13),甚至在某些“特殊”情况下还包括G(s))的活性来调节信号级联反应,从而引起膜脂代谢、蛋白激酶及其靶点的磷酸化状态、单体G蛋白的激活状态以及包括cAMP、Ca(2+)离子、脂肪酸和其他小分子在内的细胞内第二信使水平的变化。根据其表达位点和可用的信号通路,CaR可调节细胞增殖与存活、分化、肽激素分泌、离子和水运输以及各种其他过程。在本文中,我们探讨了CaR引发其细胞功能的复杂细胞内机制。我们还探讨了一些已被更好理解的CaR调节的细胞功能以及支持这些功能的信号机制的本质。