TY - JOUR
T1 - Salusin β is a surrogate ligand of the mas-like G protein-coupled receptor MrgA1
AU - Wang, Zhiwei
AU - Takahashi, Toshio
AU - Saito, Yumiko
AU - Nagasaki, Hiroshi
AU - Ly, Nga Kim
AU - Nothacker, Hans Peter
AU - Reinscheid, Rainer K.
AU - Yang, Jun
AU - Chang, Jaw Kang
AU - Shichiri, Masayoshi
AU - Civelli, Olivier
PY - 2006/6/13
Y1 - 2006/6/13
N2 - 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 β activates the mouse mas-like G protein-coupled receptor, mMrgA1 with an EC50 of about 300 nM. Salusin β 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 β does not activate corresponding human mas-like G protein-coupled receptors. Our results show that human salusin β 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.
AB - 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 β activates the mouse mas-like G protein-coupled receptor, mMrgA1 with an EC50 of about 300 nM. Salusin β 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 β does not activate corresponding human mas-like G protein-coupled receptors. Our results show that human salusin β 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.
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U2 - 10.1016/j.ejphar.2006.03.064
DO - 10.1016/j.ejphar.2006.03.064
M3 - Article
C2 - 16697365
AN - SCOPUS:33646883475
VL - 539
SP - 145
EP - 150
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 3
ER -