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广谱氨基酸感应型 C 类 G 蛋白偶联受体:分子机制、生理意义及药物研发选择。

Broad-spectrum amino acid-sensing class C G-protein coupled receptors: molecular mechanisms, physiological significance and options for drug development.

机构信息

School of Molecular Bioscience (G08), University of Sydney, NSW 2006, Australia.

出版信息

Pharmacol Ther. 2010 Sep;127(3):252-60. doi: 10.1016/j.pharmthera.2010.04.007. Epub 2010 May 6.

Abstract

In this article, we consider the molecular mechanisms that underlie broad-spectrum amino acid sensing by a discrete subgroup of class C G-protein-coupled receptors that includes the calcium-sensing receptor, GPRC6A and heterodimers composed of two closely related receptor subunits, T1R(1) and T1R(3). We consider their physiological significance highlighting their diverse spectrum of cellular responses and the phenotypes of global and conditional knock-out mice. In addition, we consider strategies for the development of new drugs that target these receptors.

摘要

在本文中,我们考虑了广泛的氨基酸感应的分子机制,该机制由包括钙敏感受体、GPRC6A 以及由两个密切相关的受体亚基 T1R(1)和 T1R(3)组成的异源二聚体在内的一类 C 族 G 蛋白偶联受体的一个离散亚群所介导。我们考虑了它们的生理意义,强调了它们在细胞反应谱上的多样性,以及全局和条件敲除小鼠的表型。此外,我们还考虑了针对这些受体的新药开发策略。

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