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综述:治疗药物对 Mas 相关 G 蛋白偶联受体 X2 的激活作用。

Minireview: Mas-related G protein-coupled receptor X2 activation by therapeutic drugs.

机构信息

Feinberg Department of Medicine, Division of Allergy & Immunology, Northwestern University, McGaw M-301 240 E Huron St. Chicago, Chicago, IL, 60611, USA.

出版信息

Neurosci Lett. 2021 Apr 23;751:135746. doi: 10.1016/j.neulet.2021.135746. Epub 2021 Feb 18.

Abstract

Symptoms that resemble allergic reactions, such as pruritus, flushing, and hypotension, are common side effects of therapeutic drugs. In a true allergic reaction, Immunoglobulin E (IgE) antibodies recognize the drug and trigger mediator release from mast cells through cross-linking of IgE receptors. However, many drugs can bypass this pathway and can activate mast cells directly through MRGPRX2, a G protein-coupled receptor that responds to a wide range of small molecules, peptides, and proteins that have little in common except for a net positive charge. This review will provide an overview of MRGPRX2, including its expression pattern, studies of its pharmacology, and its orthologs. It also will review evidence for MRGPRX2 activation by many drugs closely associated with these reactions.

摘要

类似于过敏反应的症状,如瘙痒、潮红和低血压,是治疗药物的常见副作用。在真正的过敏反应中,免疫球蛋白 E(IgE)抗体识别药物并通过 IgE 受体的交联触发肥大细胞释放介质。然而,许多药物可以绕过这条途径,并且可以通过 MRGPRX2 直接激活肥大细胞,MRGPRX2 是一种 G 蛋白偶联受体,它对广泛的小分子、肽和蛋白质作出反应,这些小分子、肽和蛋白质除了带有净正电荷外几乎没有共同之处。这篇综述将提供对 MRGPRX2 的概述,包括其表达模式、药理学研究及其同源物。它还将回顾许多与这些反应密切相关的药物通过 MRGPRX2 激活的证据。

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