ArticleBritish journal of pharmacology2013
Therapeutic potential of histamine H₄ receptor agonists in triple-negative human breast cancer experimental model.
Article in British journal of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers, 1 of them a synthesis that pooled it.
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30 citing papers in PubMed, 1 synthesis or guideline pooled it, 48 citations in OpenAlex.
- Canonical and Non-Canonical Antipsychotics' Dopamine-Related Mechanisms of Present and Next Generation Molecules: A Systematic Review on Translational Highlights for Treatment Response and Treatment-Resistant Schizophrenia.International journal of molecular sciences · 2023Pooled it
- Targeting histamine signaling: repurposing antihistamines for cancer chemotherapy and immunotherapy.Archives of pharmacal research · 2026Review
- Neurotransmitters and Immunity: Molecular Mechanisms, Biological Functions, Diseases, and Potential Therapeutic Targets.MedComm · 2025Review
- Histamine HInflammation research : official journal of the European Histamine Research Society ... [et al.] · 2025Review
- A psychiatric medication, clozapine, induces autophagy and apoptosis in breast cancer cells through reactive oxygen species.PloS one · 2025Article
- The role of histamine and its receptors in breast cancer: from pathology to therapeutic targets.Medical oncology (Northwood, London, England) · 2024Review
- Nanomicellar Formulations Loaded with Histamine and Paclitaxel as a New Strategy to Improve Chemotherapy for Breast Cancer.International journal of molecular sciences · 2023Article
- Breast cancer and neurotransmitters: emerging insights on mechanisms and therapeutic directions.Oncogene · 2023Review
- HTR1A Inhibits the Progression of Triple-Negative Breast Cancer via TGF-β Canonical and Noncanonical Pathways.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Article
- Histamine H4 Receptor Expression in Triple-negative Breast Cancer: An Exploratory Study.The journal of histochemistry and cytochemistry : official journal of the Histochemistry Society · 2022Article
- Histamine H4 Receptor Agonism Induces Antitumor Effects in Human T-Cell Lymphoma.International journal of molecular sciences · 2022Article
- Histamine in cancer immunology and immunotherapy. Current status and new perspectives.Pharmacology research & perspectives · 2021Review
- Pathophysiological Roles of Histamine Receptors in Cancer Progression: Implications and Perspectives as Potential Molecular Targets.Biomolecules · 2021Review
- Granulocytes and Cells of Granulocyte Origin-The Relevant Players in Colorectal Cancer.International journal of molecular sciences · 2021Review
- Histamine, Metabolic Remodelling and Angiogenesis: A Systems Level Approach.Biomolecules · 2021Review
- Article
- Circulating basophil count as a prognostic marker of tumor aggressiveness and survival outcomes in colorectal cancer.Clinical and translational medicine · 2020Article
- Study of the antitumour effects and the modulation of immune response by histamine in breast cancer.British journal of cancer · 2020Article
- Histamine receptors and cancer pharmacology: an update.British journal of pharmacology · 2020Review
- Commentary: Pathophysiological Role of Histamine H4 Receptor in Cancer: Therapeutic Implications.Frontiers in pharmacology · 2020Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe presence of the histamine H₄ receptor (H₄R) was previously reported in benign and malignant lesions and cell lines derived from the human mammary gland. The aim of this work was to evaluate the effects of H₄R ligands on the survival, tumour growth rate and metastatic capacity of breast cancer in an experimental model. EXPERIMENTAL APPROACH: Xenograft tumours of the highly invasive human breast cancer cell line MDA-MB-231 were established in immune deficient nude mice. The following H₄R agonists were employed: histamine (5 mg kg⁻¹), clozapine (1 mg kg⁻¹) and the experimental compound JNJ28610244 (10 mg kg⁻¹).
resultsData indicate that developed tumours were highly undifferentiated, expressed H₄R and exhibited high levels of histamine content and proliferation marker (PCNA) while displaying low apoptosis. Mice of the untreated group displayed a median survival of 60 days and a tumour doubling time of 7.4 ± 0.6 days. A significant decrease in tumour growth evidenced by an augment of the tumour doubling time was observed in the H₄R agonist groups (13.1 ± 1.2, P < 0.01 in histamine group; 15.1 ± 1.1, P < 0.001 in clozapine group; 10.8 ± 0.7, P < 0.01 in JNJ28610244 group). This effect was associated with a decrease in the PCNA expression levels, and also reduced intratumoural vessels in histamine and clozapine treated mice. Histamine significantly increased median survival (78 days; Log rank Mantel-Cox Test, P = 0.0025; Gehan-Breslow-Wilcoxon Test, P = 0.0158) and tumoural apoptosis. CONCLUSIONS AND IMPLICATIONS: Histamine through the H₄R exhibits a crucial role in tumour progression. Therefore, H₄R ligands offer a novel therapeutic potential as adjuvants for breast cancer treatment.
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