Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells

Mast cells (MCs) act as primary effectors in inflammatory and allergic reactions by releasing intracellularly-stored inflammatory mediators in diseases. The two major pathways for MC activation are known to be immunoglobulin E (IgE)-dependent and -independent. Although IgE-dependent signaling is the...

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Autores principales:	Hiroyuki Ogasawara, Masato Noguchi
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	mast cell activation MRGPRX2 MRGPRX2 inhibitor neurogenic inflammation type 2 inflammation non-histaminergic itch Biology (General) QH301-705.5
Acceso en línea:	https://doaj.org/article/2ea13677bbc942228470c48136bd7146
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spelling	oai:doaj.org-article:2ea13677bbc942228470c48136bd71462021-11-25T17:08:46ZTherapeutic Potential of MRGPRX2 Inhibitors on Mast Cells10.3390/cells101129062073-4409https://doaj.org/article/2ea13677bbc942228470c48136bd71462021-10-01T00:00:00Zhttps://www.mdpi.com/2073-4409/10/11/2906https://doaj.org/toc/2073-4409Mast cells (MCs) act as primary effectors in inflammatory and allergic reactions by releasing intracellularly-stored inflammatory mediators in diseases. The two major pathways for MC activation are known to be immunoglobulin E (IgE)-dependent and -independent. Although IgE-dependent signaling is the main pathway to MC activation, IgE-independent pathways have also been found to serve pivotal roles in the pathophysiology of various inflammatory conditions. Recent studies have shown that human and mouse MCs express several regulatory receptors such as toll-like receptors (TLRs), CD48, C300a, and GPCRs, including mas-related GPCR-X2 (MRGPRX2). MRGPRX2 has been reported as a novel GPCR that is expressed in MCs activated by basic secretagogues, neurokinin peptides, host defense antimicrobial peptides, and small molecule compounds (e.g., neuromuscular blocking agents) and leads to MC degranulation and eicosanoids release under in vitro experimental condition. Functional analyses of MRGPRX2 and Mrgprb2 (mouse ortholog) indicate that MRGPRX2 is involved in MC hypersensitivity reactions causing neuroinflammation such as postoperative pain, type 2 inflammation, non-histaminergic itch, and drug-induced anaphylactic-like reactions. In this review, we discuss the roles in innate immunity through functional studies on MRGPRX2-mediated IgE-independent MC activation and also the therapeutic potential of MRGPRX2 inhibitors on allergic and inflammatory diseases.Hiroyuki OgasawaraMasato NoguchiMDPI AGarticlemast cell activationMRGPRX2MRGPRX2 inhibitorneurogenic inflammationtype 2 inflammationnon-histaminergic itchBiology (General)QH301-705.5ENCells, Vol 10, Iss 2906, p 2906 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	mast cell activation MRGPRX2 MRGPRX2 inhibitor neurogenic inflammation type 2 inflammation non-histaminergic itch Biology (General) QH301-705.5
spellingShingle	mast cell activation MRGPRX2 MRGPRX2 inhibitor neurogenic inflammation type 2 inflammation non-histaminergic itch Biology (General) QH301-705.5 Hiroyuki Ogasawara Masato Noguchi Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells
description	Mast cells (MCs) act as primary effectors in inflammatory and allergic reactions by releasing intracellularly-stored inflammatory mediators in diseases. The two major pathways for MC activation are known to be immunoglobulin E (IgE)-dependent and -independent. Although IgE-dependent signaling is the main pathway to MC activation, IgE-independent pathways have also been found to serve pivotal roles in the pathophysiology of various inflammatory conditions. Recent studies have shown that human and mouse MCs express several regulatory receptors such as toll-like receptors (TLRs), CD48, C300a, and GPCRs, including mas-related GPCR-X2 (MRGPRX2). MRGPRX2 has been reported as a novel GPCR that is expressed in MCs activated by basic secretagogues, neurokinin peptides, host defense antimicrobial peptides, and small molecule compounds (e.g., neuromuscular blocking agents) and leads to MC degranulation and eicosanoids release under in vitro experimental condition. Functional analyses of MRGPRX2 and Mrgprb2 (mouse ortholog) indicate that MRGPRX2 is involved in MC hypersensitivity reactions causing neuroinflammation such as postoperative pain, type 2 inflammation, non-histaminergic itch, and drug-induced anaphylactic-like reactions. In this review, we discuss the roles in innate immunity through functional studies on MRGPRX2-mediated IgE-independent MC activation and also the therapeutic potential of MRGPRX2 inhibitors on allergic and inflammatory diseases.
format	article
author	Hiroyuki Ogasawara Masato Noguchi
author_facet	Hiroyuki Ogasawara Masato Noguchi
author_sort	Hiroyuki Ogasawara
title	Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells
title_short	Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells
title_full	Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells
title_fullStr	Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells
title_full_unstemmed	Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells
title_sort	therapeutic potential of mrgprx2 inhibitors on mast cells
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/2ea13677bbc942228470c48136bd7146
work_keys_str_mv	AT hiroyukiogasawara therapeuticpotentialofmrgprx2inhibitorsonmastcells AT masatonoguchi therapeuticpotentialofmrgprx2inhibitorsonmastcells
_version_	1718412638867685376

Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells

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