Salusin β is a surrogate ligand of the mas-like G protein-coupled receptor MrgA1

Zhiwei Wang, Toshio Takahashi, Yumiko Saito, Hiroshi Nagasaki, Nga Kim Ly, Hans Peter Nothacker, Rainer K. Reinscheid, Jun Yang, Jaw Kang Chang, Masayoshi Shichiri, Olivier Civelli

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30 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)145-150
Number of pages6
JournalEuropean Journal of Pharmacology
Volume539
Issue number3
DOIs
Publication statusPublished - 13-06-2006
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Pharmacology

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    Wang, Z., Takahashi, T., Saito, Y., Nagasaki, H., Ly, N. K., Nothacker, H. P., Reinscheid, R. K., Yang, J., Chang, J. K., Shichiri, M., & Civelli, O. (2006). Salusin β is a surrogate ligand of the mas-like G protein-coupled receptor MrgA1. European Journal of Pharmacology, 539(3), 145-150. https://doi.org/10.1016/j.ejphar.2006.03.064