ArticleFrontiers in immunology2024
Pharmacological blockade of the mast cell MRGPRX2 receptor supports investigation of its relevance in skin disorders.
Article in Frontiers in immunology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Mast Cells in Neuroimmune Interactions: Mechanisms, Pathophysiological Roles, and Therapeutic Implications.Molecular neurobiology · 2026Review
- Mast cell proteases and their significance in physiology, pathology, and therapeutic approaches.Pharmacological reviews · 2026Review
- EGR1 regulates degranulation and mediator release in C48/80-induced pseudo-allergic reactions.Immunologic research · 2026Article
- Mast Cells and Substance P: Neuroinflammatory Loops at the Molecular and Translational Clinical Levels.Biomolecules · 2026Review
- Cross-Talk between Neurons and Immune Cells in Pruritus: from Mechanisms To Medicines.Current allergy and asthma reports · 2026Review
- Mas-Related G-Protein-Coupled Receptors: Emerging Roles in Neuropathic Pain.Biomolecules · 2026Review
- Advances in the Management of Mediator-Related Symptoms in Non-Advanced Systemic Mastocytosis.ImmunoTargets and therapy · 2026Review
- Nanomaterials in Targeted Immunotherapy for Chronic Spontaneous Urticaria: Focusing on Immune Cell Modulation and Precision Treatment.International journal of nanomedicine · 2026Review
- Review
- Mast Cells at the Crossroads of Hypersensitivity Reactions and Neurogenic Inflammation.International journal of molecular sciences · 2025Review
- Functional heterogeneity of mast cells in cutaneous inflammation: implications for precision medicine.Frontiers in immunology · 2025Review
- Mast cell-neuron axis as a core mechanism in chronic pruritus of atopic dermatitis: from mechanistic insights to therapeutic targets.Frontiers in immunology · 2025Review
- The development of murine bone marrow-derived mast cells expressing functional human MRGPRX2 forFrontiers in immunology · 2024Article
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Authors and funding
10 authors.
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Abstract
Introduction: Because MRGPRX2 is now recognized as the mast cell receptor for basic secretagogues, there is currently a tremendous interest in whether MRGRPX2 could play an important role in various pruritic dermatoses such as chronic spontaneous urticaria. Therefore, we sought to identify new potent and selective antagonists to pharmacologically characterize the biological role of MRGPRX2. Methods: Various relevant Results: Two novel and structurally distinct MRGPRX2 antagonists were identified with one, Compound B, being orally active and demonstrating high potency in blocking Substance P-mediated degranulation using freshly isolated human skin mast cells with half maximal inhibitory concentration (IC Conclusion: These data fully support the investigation of MRGPRX2 receptor antagonists in mast cell-driven allergic skin disorders such as chronic spontaneous urticaria.
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