Salusin beta is a surrogate ligand of the mas-like G protein-coupled receptor MrgA1.
Salusin beta is a surrogate ligand of the mas-like G protein-coupled receptor MrgA1.
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发表时间：
2006
影响因子：
5
通讯作者：
Zhiwei Wang;Toshio Takahashi;Yumiko Saito;H. Nagasaki;N. K. Ly;H. Nothacker;R. Reinscheid;Jun Yang;J. Chang;M. Shichiri;O. Civelli
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文献类型：
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作者：
Zhiwei Wang;Toshio Takahashi;Yumiko Saito;H. Nagasaki;N. K. Ly;H. Nothacker;R. Reinscheid;Jun Yang;J. Chang;M. Shichiri;O. Civelli
mas样G蛋白偶联受体形成G蛋白偶联受体的一个亚家族，其包括不同物种的可变成员数目，并且已显示结合从肽到氨基酸衍生物的多种配体。在筛选针对不同孤儿G蛋白偶联受体的肽库时，我们发现人salusin beta激活小鼠mas样G蛋白偶联受体mMrgA 1，EC（50）约为300 nM。Salusin beta是最近通过生物信息学分析发现的一种生物活性肽，它能刺激大鼠垂体释放垂体后叶素-加压素，引起迅速而严重的低血压和心动过缓。然而，当我们进一步分析mMrgA 1激活的一般性时，我们发现人salusin beta不激活相应的人mas样G蛋白偶联受体。我们的研究结果表明，人salusin β是小鼠MrgA 1的替代配体，并提出了一个警示旗的实验，分析不同物种的mas样G蛋白偶联受体的药理学概况。
The mas-like G protein-coupled receptors form a subfamily of G protein-coupled receptors that includes variable member numbers across different species and that have been shown to bind a wide variety of ligands from peptides to amino acid derivatives. While screening a library of peptides against different orphan G protein-coupled receptors, we found that human salusin beta activates the mouse mas-like G protein-coupled receptor, mMrgA1 with an EC(50) of about 300 nM. Salusin beta is a bioactive peptide recently discovered through bioinformatics analysis which stimulates arginine-vasopressin release from rat pituitary and causes rapid and profound hypotension and bradycardia. However, when we further analyzed the generality of the mMrgA1 activation, we found that human salusin beta does not activate corresponding human mas-like G protein-coupled receptors. Our results show that human salusin beta is a surrogate ligand of the mouse MrgA1 and raises a cautionary flag for experiments that analyze the pharmacological profiles of mas-like G protein-coupled receptors from different species.