ArticleThe international journal of biochemistry & cell biology2011
Structural requirements for the inhibition of calcium mobilization and mast cell activation by the pyrazole derivative BTP2.
Article in The international journal of biochemistry & cell biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 42 citations in OpenAlex.
- A Review on Pyrazole Derivatives Used in the Treatment of Rheumatoid Arthritis: Recent Advancement and Drug Development.Current rheumatology reviews · 2025Review
- 1,2,4-Oxadiazole-Bearing Pyrazoles as Metabolically Stable Modulators of Store-Operated Calcium Entry.ACS medicinal chemistry letters · 2021Article
- Development of Store-Operated Calcium Entry-Targeted Compounds in Cancer.Frontiers in pharmacology · 2021Review
- Chinese Society of Allergy Guidelines for Diagnosis and Treatment of Allergic Rhinitis.Allergy, asthma & immunology research · 2018Review
- Lipophilic Chemicals from Diesel Exhaust Particles Trigger Calcium Response in Human Endothelial Cells via Aryl Hydrocarbon Receptor Non-Genomic Signalling.International journal of molecular sciences · 2018Article
- Article
- Structure-activity relationship study and discovery of indazole 3-carboxamides as calcium-release activated calcium channel blockers.Bioorganic & medicinal chemistry letters · 2017Article
- Role of interleukin-18 in the pathophysiology of allergic diseases.Cytokine & growth factor reviews · 2016Review
- Calcium Signaling Is Dispensable for Receptor Regulation of Endothelial Barrier Function.The Journal of biological chemistry · 2016Article
- Basophil-derived IL-4 plays versatile roles in immunity.Seminars in immunopathology · 2016Review
- SOCE and cancer: Recent progress and new perspectives.International journal of cancer · 2016Review
- Store-operated CRAC channel inhibitors: opportunities and challenges.Future medicinal chemistry · 2016Review
- Cutting Edge: Drebrin-Regulated Actin Dynamics Regulate IgE-Dependent Mast Cell Activation and Allergic Responses.Journal of immunology (Baltimore, Md. : 1950) · 2015Article
- A store-operated calcium channel inhibitor attenuates collagen-induced arthritis.British journal of pharmacology · 2015Article
- Signaling pathways activated by a protease allergen in basophils.Proceedings of the National Academy of Sciences of the United States of America · 2014Article
- Mast cells and basophils are essential for allergies: mechanisms of allergic inflammation and a proposed procedure for diagnosis.Acta pharmacologica Sinica · 2013Review
- Article
- Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways.British journal of pharmacology · 2012Article
- Molecular pharmacology of store-operated CRAC channels.Channels (Austin, Tex.)Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Mast cells play a critical role in the development of the allergic response. Upon activation by allergens and IgE via the high affinity receptor for IgE (FcɛRI), these cells release histamine and other functional mediators that initiate and propagate immediate hypersensitivity reactions. Mast cells also secrete cytokines that can regulate immune activity. These processes are controlled, in whole or part, by increases in intracellular Ca(2+) induced by the FcɛRI. We show here that N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide (BTP2), a pyrazole derivative, inhibits activation-induced Ca(2+) influx in the rat basophil cell line RBL-2H3 and in bone marrow-derived mast cells (BMMCs), without affecting global tyrosine phosphorylation of cellular proteins or phosphorylation of the mitogen-activated protein kinases Erk1/2, JNK and p38. BTP2 also inhibits activation-induced degranulation and secretion of interleukin (IL)-2, IL-3, IL-4, IL-6, IL-13, tumor necrosis factor (TNF)-α, and granulocyte macrophage-colony stimulating factor (GM-CSF) by BMMCs, which correlates with the inhibition of Nuclear Factor of Activated T cells (NFAT) translocation. In vivo, BTP2 inhibits antigen-induced histamine release. Structure-activity relationship analysis indicates that substitution at the C3 or C5 position of the pyrazole moiety on BTP2 (5-trifluoromethyl-3-methyl-pyrazole or 3-trifluoromethyl-5-methyl-pyrazole, respectively) affected its activity, with the trifluoromethyl group at the C3 position being critical to its activity. We conclude that BTP2 and related compounds may be potent modulators of mast cell responses and potentially useful for the treatment of symptoms of allergic inflammation.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.