Stimulation of the extracellular Ca2+-sensing receptor by denatonium

被引：9

作者：

Rogachevskaja, Olga A. ^{[1
]}

Churbanov, Gleb D. ^{[1
]}

Bystrova, Marina F. ^{[1
]}

Romanov, Roman A. ^{[1
]}

Kolesnikov, Stanislav S. ^{[1
]}

机构：

[1] Russian Acad Sci, Inst Cell Biophys, Pushchino 142290, Moscow Region, Russia

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 2011年 / 416卷 / 3-4期

基金：

俄罗斯基础研究基金会;

关键词：

Extracellular Ca2+-sensing receptor; Ca2+ imaging; Heterologous expression; Denatonium;

D O I：

10.1016/j.bbrc.2011.11.095

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The extracellular Ca2+-sensing receptor (CASR) is a promiscuous G-protein-coupled receptor closely related to the taste receptors T1R1-T1R3. Here we analyzed the possibility that apart from being stimulated by external Ca2+ and amino acids, the substances effective as tastants, CASR might serve as a receptor for other sapid compounds. CASR was heterologously expressed in HEK-293 cells, and their responsivity to a variety of bitter and sweet substances was examined. Among them, solely denatonium was found to stimulate Ca2+ signaling in CASR-positive HEK-293 cells. Apparently, these Ca2+ responses were specific, as those were inhibited by the CASR antagonist NSP-4123. Altogether, our findings indicate that denatonium stimulates CASR by shifting a dose-response curve for the principal CASR agonist Ca2+ to lower concentrations. (C) 2011 Elsevier Inc. All rights reserved.

引用

页码：433 / 436

页数：4

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