ArticleNaunyn-Schmiedeberg's archives of pharmacology2014
Terfenadine induces anti-proliferative and apoptotic activities in human hormone-refractory prostate cancer through histamine receptor-independent Mcl-1 cleavage and Bak up-regulation.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 34 citations in OpenAlex.
- Targeting histamine signaling: repurposing antihistamines for cancer chemotherapy and immunotherapy.Archives of pharmacal research · 2026Review
- Antihistamine drug terfenadine suppressed the cycle progression of gastric cancer cells by targeting PI3K/AKT/mTOR signaling.Frontiers in pharmacology · 2026Article
- Combinatorial Anti-Mitotic Activity of Loratadine/5-Fluorouracil Loaded Zein Tannic Acid Nanoparticles in Breast Cancer Therapy: In silico, in vitro and Cell Studies.International journal of nanomedicine · 2026Article
- The Road to Precision Nanomedicine: An Insight on Drug Repurposing and Advances in Nanoformulations for Treatment of Cancer.AAPS PharmSciTech · 2025Review
- Underlying Mechanism of Lysosomal Membrane Permeabilization in CNS Injury: A Literature Review.Molecular neurobiology · 2025Review
- Loratadine Loaded Chitosan Tannic Acid Nanoparticles as Anti-Proliferative Agent Against Breast Cancer: In-silico, in-vitro and Cell Studies.International journal of nanomedicine · 2024Article
- Terfenadine, a histamine H1 receptor antagonist, induces apoptosis by suppressing STAT3 signaling in human colorectal cancer HCT116 cells.Frontiers in pharmacology · 2024Article
- Article
- The Multidirectional Effect of Azelastine Hydrochloride on Cervical Cancer Cells.International journal of molecular sciences · 2022Article
- Identification of hub genes associated with COVID-19 and idiopathic pulmonary fibrosis by integrated bioinformatics analysis.PloS one · 2022Article
- Huanglianjiedu Decoction as an effective treatment for oral squamous cell carcinoma based on network pharmacology and experimental validation.Cancer cell international · 2021Article
- Pathophysiological Roles of Histamine Receptors in Cancer Progression: Implications and Perspectives as Potential Molecular Targets.Biomolecules · 2021Review
- Molecular genomic features associated with in vitro response of the NCI-60 cancer cell line panel to natural products.Molecular oncology · 2021Article
- Dual lysosomal-mitochondrial targeting by antihistamines to eradicate leukaemic cells.EBioMedicine · 2019Article
- Inhibition of histamine receptor H3R suppresses prostate cancer growth, invasion and increases apoptosis via the AR pathway.Oncology letters · 2018Article
- Ectopic hTERT expression facilitates reprograming of fibroblasts derived from patients with Werner syndrome as a WS cellular model.Cell death & disease · 2018Article
- Leukemic stem cell signatures identify novel therapeutics targeting acute myeloid leukemia.Blood cancer journal · 2018Article
- Cimetidine and Clobenpropit Attenuate Inflammation-Associated Colorectal Carcinogenesis in Male ICR Mice.Cancers · 2016Article
- An Investigation of the Growth Inhibitory Capacity of Several Medicinal Plants From Iran on Tumor Cell Lines.Iranian journal of cancer prevention · 2015Article
- Article
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
Although the results of several studies have underscored the regulatory effect of H1-histamine receptors in cell proliferation of some cancer cell types, its effect in prostate cancers remains unclear. We have therefore studied the effect of terfenadine (an H1-histamine receptor antagonist) in prostate cancer cell lines. Our data demonstrate that terfenadine was effective against PC-3 and DU-145 cells (two prostate cancer cell lines). In contrast, based on the sulforhodamine B assay, loratadine had less potency while fexofenadine and diphenhydramine had little effect. Terfenadine induced the cleavage of Mcl-1 cleavage into a pro-apoptotic 28-kDa fragment and up-regulation of Bak, resulting in the loss of mitochondrial membrane potential (ΔΨm) and the release of cytochrome c and apoptosis-inducing factor into the cytosol. The activation of caspase cascades was detected to be linked to terfenadine action. Bak up-regulation was also examined at both the transcriptional and translational levels, and Bak activation was validated based on conformational change to expose the N terminus. Terfenadine also induced an indirect-but not direct-DNA damage response through the cleavage and activation of caspase-2, phosphorylation and activation of Chk1 and Chk2 kinases, phosphorylation of RPA32 and acetylation of Histone H3; these processes were highly correlated to severe mitochondrial dysfunction and the activation of caspase cascades. In conclusion, terfenadine induced apoptotic signaling cascades against HRPCs in a sequential manner. The exposure of cells to terfenadine caused the up-regulation and activation of Bak and the cleavage of Mcl-1, leading to the loss of ΔΨm and activation of caspase cascades which further resulted in DNA damage response and cell apoptosis.
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