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Updated: May 17, 2026

Screening Peptides that Activate MRGPRX2 using Engineered HEK Cells
Published on: November 6, 2021
Identification of physiologically active substances as novel ligands for MRGPRD
Makiko Uno1, Satoko Nishimura, Keisuke Fukuchi
1Exploratory Research Laboratories II, Daiichi Sankyo Co, Ltd, Tokyo 134-8630, Japan. uno.makiko.mv@daiichisankyo.co.jp
Abstract:
Mas-related G-protein coupled receptor member D (MRGPRD) is a G protein-coupled receptor (GPCR) which belongs to the Mas-related GPCRs expressed in the dorsal root ganglia (DRG). In this study, we investigated two novel ligands in addition to beta-alanine: (1) beta-aminoisobutyric acid, a physiologically active substance, with which possible relation to tumors has been seen together with beta-alanine; (2) diethylstilbestrol, a synthetic estrogen hormone. In addition to the novel ligands, we found that transfection of MRGPRD leads fibroblast cells to form spheroids, which would be related to oncogenicity. To understand the MRGPRD novel character, oncogenicity, a large chemical library was screened in order to obtain MRGPRD antagonists to utilize in exploring the character. The antagonist in turn inhibited the spheroid proliferation that is dependent on MRGPRD signaling as well as MRGPRD signals activated by beta-alanine. The antagonist, a small-molecule compound we found in this study, is a potential anticancer agent.
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