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

研究成果: Article査読

32 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)145-150
ページ数6
ジャーナルEuropean Journal of Pharmacology
539
3
DOI
出版ステータスPublished - 13-06-2006
外部発表はい

All Science Journal Classification (ASJC) codes

  • Pharmacology

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