无结构环对于 mGluR2 的激活是必需的。

Unstructured loop is essential for the activation of mGluR2.

机构信息

Department of Biochemistry, Weill Cornell Medical College, New York City, NY, USA; Department of Cell and Molecular Physiology, Stritch School of Medicine, Maywood, IL, USA.

Cell and Developmental Biology Center, National Heart, Lung and Blood Institute, National Institutes of Health, Bethesda, MD, USA.

出版信息

Biochem Biophys Res Commun. 2020 Jan 15;521(3):775-778. doi: 10.1016/j.bbrc.2019.10.187. Epub 2019 Nov 6.

DOI:10.1016/j.bbrc.2019.10.187

PMID:31706572

Abstract

Metabotropic Glutamate Receptors (mGluRs) are Class C G-protein coupled receptors (GPCRs) that are expressed throughout the central nervous system and are involved in several neurological and psychiatric disorders. Although, many studies focused on Glutamate induced activation of mGluR2, however, the role of unstructured loop (or "BC loop") in activation of metabotropic Glutamate receptors is currently unknown. Here, using Förster Resonance Energy Transfer (FRET) based assay in live cells we show that unstructured loop is required for Glutamate induced conformation and hence the activation of the receptor.

摘要

代谢型谷氨酸受体（mGluRs）是 C 类 G 蛋白偶联受体（GPCRs），广泛表达于中枢神经系统，参与多种神经和精神疾病。虽然许多研究集中在谷氨酸诱导的 mGluR2 激活上，但无规卷曲（或“BC 环”）在代谢型谷氨酸受体激活中的作用目前尚不清楚。在这里，我们在活细胞中使用荧光共振能量转移（FRET）测定法表明，无规卷曲对于谷氨酸诱导的构象变化以及受体的激活是必需的。