Icatibant Acts as a Balanced Ligand of MRGPRX2 in Human Skin Mast Cells

MRGPRX2 (Mas-related G protein-coupled receptor member X2) is implicated in mast cell (MC)-driven disorders due to its ability to bind diverse ligands, which may be G-protein-biased or balanced, with the latter activating both G-proteins and the β-arrestin pathway. Icatibant, a peptide drug, produce...

Full description

Bibliographic Details
Published in:	Biomolecules
Main Authors:	Zhuoran Li, Jean Schneikert, Gürkan Bal, Torsten Zuberbier, Magda Babina
Format:	Article
Language:	English
Published:	MDPI AG 2025-08-01
Subjects:	mast cells MRGPRX2 degranulation icatibant drug allergy desensitization
Online Access:	https://www.mdpi.com/2218-273X/15/9/1224

Similar Items

A Novel Cell Culture System to Improve MRGPRX2 Research in Human Skin Mast Cells
by: Zhuoran Li, et al.
Published: (2025-10-01)

CREB Is Critically Implicated in Skin Mast Cell Degranulation Elicited via FcεRI and MRGPRX2
by: Zhuoran Li, et al.
Published: (2024-10-01)

MRGPRX2-Mediated Degranulation of Human Skin Mast Cells Requires the Operation of G<sub>αi</sub>, G<sub>αq</sub>, Ca++ Channels, ERK1/2 and PI3K—Interconnection between Early and Late Signaling
by: Zhao Wang, et al.
Published: (2022-03-01)

Thymic Stromal Lymphopoietin Promotes MRGPRX2-Triggered Degranulation of Skin Mast Cells in a STAT5-Dependent Manner with Further Support from JNK
by: Magda Babina, et al.
Published: (2021-01-01)

Neuronal substance P-driven MRGPRX2-dependent mast cell degranulation products differentially promote vascular permeability
by: Masakazu Nagamine, et al.
Published: (2024-11-01)

Quercetin Attenuates MRGPRX2-Mediated Mast Cell Degranulation via the MyD88/IKK/NF-κB and PI3K/AKT/ Rac1/Cdc42 Pathway
by: Zhao C, et al.
Published: (2024-10-01)

Synergism between IL-33 and MRGPRX2/FcεRI Is Primarily Due to the Complementation of Signaling Modules, and Only Modestly Supplemented by Prolonged Activation of Selected Kinases
by: Kristin Franke, et al.
Published: (2023-11-01)

Activation of ryanodine-sensitive calcium store drives pseudo-allergic dermatitis via Mas-related G protein-coupled receptor X2 in mast cells
by: Zhao Wang, et al.
Published: (2023-06-01)

MRGPRX2 signaling involves the Lysyl-tRNA synthetase and MITF pathway
by: Yanru Guo, et al.
Published: (2023-05-01)

Authentic and Ectopically Expressed MRGPRX2 Elicit Similar Mechanisms to Stimulate Degranulation of Mast Cells
by: Pia Lazki-Hagenbach, et al.
Published: (2021-02-01)

Mutations of MRGPRX2, drug sensitivity, and genetic markers related to disease
by: Subashini Hemamala Ratnayake, MSc, BSc, et al.
Published: (2025-08-01)

Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells
by: Hiroyuki Ogasawara, et al.
Published: (2021-10-01)

An optimized method for IgE-mediated degranulation of human lung mast cells
by: Yitao Gong, et al.
Published: (2024-05-01)

Pharmacological blockade of the mast cell MRGPRX2 receptor supports investigation of its relevance in skin disorders
by: Colin H. Macphee, et al.
Published: (2024-10-01)

Beyond Allergies—Updates on The Role of Mas-Related G-Protein-Coupled Receptor X2 in Chronic Urticaria and Atopic Dermatitis
by: Liron Lerner, et al.
Published: (2024-01-01)

In the skin lesions of patients with mycosis fungoides, the number of MRGPRX2-expressing cells is increased and correlates with mast cell numbers
by: Man Hu, et al.
Published: (2023-10-01)

Effect of icatibant on sweating-induced dermal pain
by: Shunsuke Takahagi, et al.
Published: (2025-02-01)

The Underlying Rab Network of MRGPRX2-Stimulated Secretion Unveils the Impact of Receptor Trafficking on Secretory Granule Biogenesis and Secretion
by: Pia Lazki-Hagenbach, et al.
Published: (2024-01-01)

MRGPRX2 Activation by Rocuronium: Insights from Studies with Human Skin Mast Cells and Missense Variants
by: Chalatip Chompunud Na Ayudhya, et al.
Published: (2021-01-01)

CREB Is Indispensable to KIT Function in Human Skin Mast Cells—A Positive Feedback Loop between CREB and KIT Orchestrates Skin Mast Cell Fate
by: Gürkan Bal, et al.
Published: (2023-12-01)

Functional MRGPRX2 expression on peripheral blood-derived human mast cells increases at low seeding density and is suppressed by interleukin-9 and fetal bovine serum
by: Toon Ieven, et al.
Published: (2024-12-01)

Research Progress of Icatibant in the Treatment of Hereditary Angioedema
by: XU Yanhua, et al.
Published: (2025-07-01)

Breakthrough attacks in patients with hereditary angioedema receiving long-term prophylaxis are responsive to icatibant: findings from the Icatibant Outcome Survey
by: Werner Aberer, et al.
Published: (2017-07-01)

Substance P analogs devoid of key residues fail to activate human mast cells via MRGPRX2
by: Shammy Raj, et al.
Published: (2023-05-01)

Human placental extract suppresses mast cell activation and induces mast cell apoptosis
by: Tongqian Wu, et al.
Published: (2023-11-01)

The development of murine bone marrow-derived mast cells expressing functional human MRGPRX2 for ex vivo and in vivo studies
by: Maram Bawazir, et al.
Published: (2024-12-01)

GRK2 inhibitors, paroxetine and CCG258747, attenuate IgE-mediated anaphylaxis but activate mast cells via MRGPRX2 and MRGPRB2
by: Monica Thapaliya, et al.
Published: (2022-10-01)

Mast cells in Health and Disease: A Review
by: P Sharada, et al.
Published: (2006-01-01)

PENGARUH EKSTRAK KULIT BUAH NAGA MERAH (HYLOCEREUS POLYRHIZUZ) DALAM MENGHAMBAT DEGRANULASI SEL MAST DAN MENCIT PUTIH JANTAN YANG TERSENSITISASI AKTIF
by: Relin Yesika, et al.
Published: (2023-03-01)

Modulation of the Mas-Related G Protein-Coupled Receptor X2 (MRGPRX2) by Xenobiotic Compounds and Its Relevance to Human Diseases
by: Alicja Dziadowiec, et al.
Published: (2024-03-01)

Amber Extract Suppressed Mast Cell-Mediated Allergic Inflammation via the Regulation of Allergic Mediators—An In Vitro Study
by: Redoyan Refli, et al.
Published: (2023-01-01)

MAST CELLS, THE EFFECTOR CELLS OF IgE-MEDIATED ALLERGY
by: Georgi Nikolov, et al.
Published: (2025-09-01)

Review of icatibant use in the Winnipeg Regional Health Authority
by: George Cai, et al.
Published: (2020-11-01)

Clorfl86/RHEX Is a Negative Regulator of SCF/KIT Signaling in Human Skin Mast Cells
by: Kristin Franke, et al.
Published: (2023-05-01)

Spike proteins of coronaviruses activate mast cells for degranulation via stimulating Src/PI3K/AKT/Ca2+ intracellular signaling cascade
by: Shuang Zhang, et al.
Published: (2025-05-01)

Inhibition of mast cell activation via MRGPRX2 receptor by Curcuma mangga and Sonchus arvensis water suspensions: An in vitro study
by: MUHAMMAD Sahid, et al.
Published: (2025-09-01)

Novel Approaches in the Inhibition of IgE-Induced Mast Cell Reactivity in Food Allergy
by: Chiara Tontini, et al.
Published: (2021-08-01)

Development of gastro-food allergy model in shrimp allergen extract-induced sensitized mice promotes mast cell degranulation
by: Honey D. Marhaeny, et al.
Published: (2023-03-01)

Mas-related G protein-coupled receptor MRGPRX2 in human basophils: Expression and functional studies
by: Alessandro Toscano, et al.
Published: (2023-01-01)

FcεRI: A Master Regulator of Mast Cell Functions
by: Yuka Nagata, et al.
Published: (2022-02-01)