N-arachidonoyl glycine, another endogenous agonist of GPR55.
N-arachidonoyl glycine, another endogenous agonist of GPR55.
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n-芳基多烯酰基甘氨酸，GPR55的另一种内源性激动剂。
DOI：
10.1016/j.bbrc.2017.07.038
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发表时间：
2017-09-02
影响因子：
3.1
通讯作者：
Abood ME
中科院分区：
文献类型：
--
作者：
Console-Bram L;Ciuciu SM;Zhao P;Zipkin RE;Brailoiu E;Abood ME
脂氨基酸作为G蛋白偶联受体的内源性调节剂，由于其参与多种生理过程而引起了人们的兴趣。特别是，这些氨基酸结合物的作用已经出现在内源性大麻素系统中。本文研究了N-花生四烯酰甘氨酸(NAGLY)对候选内源性大麻素受体GPR55的影响。我们的新发现表明，nAGLY诱导HAGPR55/CHO细胞钙动员和丝裂原活化蛋白激酶活性的浓度依赖性增加。这些增加被选择性GPR55拮抗剂ML193(N-[4-[[(3，4-Dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6，8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide)，支持受体介导的信号转导减弱。据我们所知，这是第一个将GPR55确定为内源性脂氨基酸nAGLY靶标的报告。
Interest in lipoamino acids as endogenous modulators of G-protein coupled receptors has escalated due to their involvement in a variety of physiologic processes. In particular, a role for these amino acid conjugates has emerged in the endocannabinoid system. The study presented herein investigated the effects of N-arachidonoyl glycine (NAGly) on a candidate endocannabinoid receptor, GPR55. Our novel findings reveal that NAGly induces concentration dependent increases in calcium mobilization and mitogen-activated protein kinase activities in HAGPR55/CHO cells. These increases were attenuated by the selective GPR55 antagonist ML193 (N-[4-[[(3,4-Dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide), supporting receptor mediated signaling. To our knowledge this is the first report identifying GPR55 as a target of the endogenous lipoamino acid, NAGly.
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影响因子：
2.4
作者：
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通讯作者：
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