ArticleScientific reports2016
The human organic cation transporter OCT1 mediates high affinity uptake of the anticancer drug daunorubicin.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 51 citations in OpenAlex.
- Increased MYB alternative promoter usage induces daunorubicin resistance in human leukemia cells via ABCA2 upregulation.Molecular biology reports · 2026Article
- Engineered microalgal extracellular vesicles for efficient doxorubicin delivery and improved therapeutic efficacy in breast cancer.Materials today. Bio · 2026Article
- Role of solute carrier transporters in the biodistribution and toxicity of chemotherapeutic drugs.Pharmacological reviews · 2026Review
- Dysfunction of the carnitine cycle in tumor progression.Heliyon · 2024Review
- Functional Validation of Doxorubicin-Induced Cardiotoxicity-Related Genes.JACC. CardioOncology · 2024Article
- Mechanisms of Regulation of the Expression of miRNAs and lncRNAs by Metformin in Ovarian Cancer.Pharmaceuticals (Basel, Switzerland) · 2023Review
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- Clinical Significance of Carnitine in the Treatment of Cancer: From Traffic to the Regulation.Oxidative medicine and cellular longevity · 2023Review
- Organelle-Selective Membrane Labeling through Phospholipase D-Mediated Transphosphatidylation.JACS Au · 2022Article
- Ratiometric imaging of minor groove binders in mammalian cells using Raman microscopy.RSC chemical biology · 2022Article
- Imaging and Editing the Phospholipidome.Accounts of chemical research · 2022Review
- Solute Carrier Transportome in Chemotherapy-Induced Adverse Drug Reactions.Reviews of physiology, biochemistry and pharmacology · 2022Article
- Expression and Functional Contribution of Different Organic Cation Transporters to the Cellular Uptake of Doxorubicin into Human Breast Cancer and Cardiac Tissue.International journal of molecular sciences · 2021Article
- Article
- The therapeutic importance of acid-base balance.Biochemical pharmacology · 2021Review
- The Impact of Genetic Polymorphisms in Organic Cation Transporters on Renal Drug Disposition.International journal of molecular sciences · 2020Review
- Cordycepin Resensitizes T24R2 Cisplatin-Resistant Human Bladder Cancer Cells to Cisplatin by Inactivating Ets-1 Dependent MDR1 Transcription.International journal of molecular sciences · 2020Article
- Review
- Combination of chemotherapy and physical plasma elicits melanoma cell death via upregulation of SLC22A16.Cell death & disease · 2018Article
- Metformin prevents nerve growth factor-dependent proliferative and proangiogenic effects in epithelial ovarian cancer cells and endothelial cells.Therapeutic advances in medical oncology · 2018Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
Anthracyclines such as daunorubicin are anticancer agents that are transported into cells, and exert cytotoxicity by blocking DNA metabolism. Although there is evidence for active uptake of anthracyclines into cells, the specific transporter involved in this process has not been identified. Using the high-grade serous ovarian cancer cell line TOV2223G, we show that OCT1 mediated the high affinity (Km ~ 5 μM) uptake of daunorubicin into the cells, and that micromolar amounts of choline completely abolished the drug entry. OCT1 downregulation by shRNA impaired daunorubicin uptake into the TOV2223G cells, and these cells were significantly more resistant to the drug in comparison to the control shRNA. Transfection of HEK293T cells, which accommodated the ectopic expression of OCT1, with a plasmid expressing OCT1-EYFP showed that the transporter was predominantly localized to the plasma membrane. These transfected cells exhibited an increase in the uptake of daunorubicin in comparison to control cells transfected with an empty EYFP vector. Furthermore, a variant of OCT1, OCT1-D474C-EYFP, failed to enhance daunorubicin uptake. This is the first report demonstrating that human OCT1 is involved in the high affinity transport of anthracyclines. We postulate that OCT1 defects may contribute to the resistance of cancer cells treated with anthracyclines.
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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 OpenQuestion graph.