Issue 37, 2021

Design, synthesis, and evaluation of substance P analogue with potential anti-pseudoallergic activity

Abstract

Mast cells (MCs) are innate immune cells that can cause allergic reactions. Pseudo-allergic reactions are a type of reaction that have the clinical symptoms of an allergy without involving the IgE pathway of immune MCs. Some studies have found that the MRGPRX2 is crucial for mediating such allergic reactions, as some antagonists and agonists have the same binding sites. One promising direction is to use the endogenous agonist of the receptor as a competitive inhibitor through structural modifications. Substance P induces mast cell activation through the MRGPRX2. Therefore, we designed and synthesized a new substance P analogue, and a β-hexaminosidase assay and Ca2+ mobilization assay were performed to evaluate the anti-allergic effect of the substance P analogue, while its binding characteristic to MRGPRX2 was analyzed by molecular docking and cell membrane chromatography. The results suggest that the substance P analogue could be a potential therapeutic agent for managing pseudo-allergic reactions.

Graphical abstract: Design, synthesis, and evaluation of substance P analogue with potential anti-pseudoallergic activity

Article information

Article type
Paper
Submitted
04 Jun 2021
Accepted
18 Aug 2021
First published
02 Sep 2021

New J. Chem., 2021,45, 17584-17591

Design, synthesis, and evaluation of substance P analogue with potential anti-pseudoallergic activity

X. Wang, J. Lu, T. Zhang, S. Ge, Y. Lv, Y. Hou, X. Yang, C. Wang and H. He, New J. Chem., 2021, 45, 17584 DOI: 10.1039/D1NJ02751D

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