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

•Mast cell activation is linked to common drug side effects, including pain and itch.•Many of these drugs can activate mast cells directly through the receptor MRGPRX2.•MRGPRX2 antagonists may be a novel way to reduce these symptoms. Symptoms that resemble allergic reactions, such as pruritus, flush...

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Bibliographic Details
Published in:Neuroscience letters 2021-04, Vol.751, p.135746-135746, Article 135746
Main Author: McNeil, Benjamin D.
Format: Article
Language:English
Subjects:
Analgesics - pharmacology
Analgesics - therapeutic use
Anaphylaxis
Animals
Antipruritics - pharmacology
Antipruritics - therapeutic use
Drug Hypersensitivity - drug therapy
Drug Hypersensitivity - metabolism
Flare
Humans
IgE-independent
Immediate hypersensitivity
Mast cells
Mast Cells - drug effects
Mast Cells - metabolism
Mrgprb2
MRGPRX2
Nerve Tissue Proteins - antagonists & inhibitors
Nerve Tissue Proteins - genetics
Nerve Tissue Proteins - metabolism
Pruritus
Pseudo-allergic
Receptors, G-Protein-Coupled - antagonists & inhibitors
Receptors, G-Protein-Coupled - genetics
Receptors, G-Protein-Coupled - metabolism
Receptors, Neuropeptide - antagonists & inhibitors
Receptors, Neuropeptide - genetics
Receptors, Neuropeptide - metabolism
Wheal
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Summary:•Mast cell activation is linked to common drug side effects, including pain and itch.•Many of these drugs can activate mast cells directly through the receptor MRGPRX2.•MRGPRX2 antagonists may be a novel way to reduce these symptoms. 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.
ISSN:0304-3940
1872-7972
DOI:10.1016/j.neulet.2021.135746