ArticleJournal of breast cancer2014
Transient receptor potential vanilloid 1 expression and functionality in mcf-7 cells: a preliminary investigation.
Article in Journal of breast cancer, 2014. 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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Who cites it
19 citing papers in PubMed, 33 citations in OpenAlex.
- Capsaicin enhances chemosensitivity and mitigates MMP11-driven aggressiveness in human bladder cancer.Cancer cell international · 2026Article
- The Role of the Endocannabinoid System in Oncology and the Potential Use of Cannabis Derivatives for Cancer Management in Companion Animals.Animals : an open access journal from MDPI · 2025Review
- TRPV1-Dependent Antiproliferative Activity of DioeciousInternational journal of molecular sciences · 2024Article
- Doxorubicin-Loaded Lipid Nanoparticles Coated with Calcium Phosphate as a Potential Tool in Human and Canine Osteosarcoma Therapy.Pharmaceutics · 2022Article
- TRPV1 Receptor Identification in Bovine and Canine Mitral Valvular Interstitial Cells.Veterinary sciences · 2021Article
- TRPV Protein Family-From Mechanosensing to Cancer Invasion.Biomolecules · 2021Review
- Anticarcinogenic Effects of Odorant Substances Citral, Citrathal R and Cyclovertal on Breast Cancer in vitro.Breast cancer (Dove Medical Press) · 2021Article
- Calcium Entry through TRPV1: A Potential Target for the Regulation of Proliferation and Apoptosis in Cancerous and Healthy Cells.International journal of molecular sciences · 2020Review
- Transient receptor potential cation channel subfamily V and breast cancer.Laboratory investigation; a journal of technical methods and pathology · 2020Review
- Ion Channel Signature in Healthy Pancreas and Pancreatic Ductal Adenocarcinoma.Frontiers in pharmacology · 2020Review
- Estrogenic, Antiestrogenic and Antiproliferative Activities ofNutrients · 2019Article
- Cannabinoids in cancer treatment: Therapeutic potential and legislation.Bosnian journal of basic medical sciences · 2019Review
- Anticancer Activity of Natural and Synthetic Capsaicin Analogs.The Journal of pharmacology and experimental therapeutics · 2018Review
- 5-Fluorouracil-induced mitochondrial oxidative cytotoxicity and apoptosis are increased in MCF-7 human breast cancer cells by TRPV1 channel activation but not Hypericum perforatum treatment.Molecular and cellular biochemistry · 2018Article
- Intracellular aggregated TRPV1 is associated with lower survival in breast cancer patients.Breast cancer (Dove Medical Press) · 2018Article
- Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels.PloS one · 2017Article
- Role of TRP ion channels in cancer and tumorigenesis.Seminars in immunopathology · 2016Review
- Synergic Effects of Doxorubicin and Melatonin on Apoptosis and Mitochondrial Oxidative Stress in MCF-7 Breast Cancer Cells: Involvement of TRPV1 Channels.The Journal of membrane biology · 2016Article
- Expression and functionality of TRPV1 in breast cancer cells.Breast cancer (Dove Medical Press) · 2016Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTransient receptor potential vanilloid 1 (TRPV1) is a nonselective cation channel belonging to the transient receptor potential family, and it is expressed in different neoplastic tissues. Its activation is associated with regulation of cancer growth and progression. The aim of this research was to study the expression and pharmacological characteristics of TRPV1 in cells derived from human breast cancer MCF-7 cells.
methodsTRPV1 presence was assessed by binding studies and Western blotting. Receptor binding characteristics were evaluated through competition assays, while 3-(4,5-dimethylthiazol-2-yl)-2,5,-dipheyltetrazolium bromide reduction assays were performed to confirm an early hypothesis regarding the modulation of cancer cell proliferation. The functionality of TRPV1 was evaluated by measuring Ca(2+) uptake in the presence of increasing concentrations of TRPV1 agonists and antagonists.
resultsBinding studies identified a single class of TRPV1 (Bmax 1,492±192 fmol/mg protein), and Western blot showed a signal at 100 kDa corresponding to the molecular weight of human TRPV1. Among the different tested agonists and antagonists, anandamide (Ki: 2.8×10(-11) M) and 5-iodoresiniferatoxin (5-I-RTX) (Ki: 5.6×10(-11) M) showed the highest degrees of affinity for TRPV1, respectively. All tested TRPV1 agonists and antagonists caused a significant (p<0.05) decrease in cell growth rate in MCF-7 cells. For agonists and antagonists, the efficacy of tested compounds displayed the following rank order: resiniferatoxin>anandamide>capsaicin and 5-I-RTX=capsazepine, respectively.
conclusionThese data indicate that both TRPV1 agonists and antagonists induce significant inhibition of MCF-7 cell growth. Even though the mechanisms involved in the antiproliferative effects of TRPV1 agonists and antagonists should be further investigated, it has been suggested that agonists cause desensitization of the receptor, leading to alteration in Ca(2+)-influx regulation. By contrast, antagonists cause a functional block of the receptor with consequent fatal dysregulation of cell homeostasis.
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