ArticlePloS one2017
Dicumarol inhibits PDK1 and targets multiple malignant behaviors of ovarian cancer cells.
Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed, 98 citations in OpenAlex.
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- The Mechanisms of Ramulus Cinnamomi and Rhizoma Paridis in Gynecological Cancers: A Narrative Review.Cancer management and research · 2026Review
- Glycolytic reprogramming in ovarian cancer: mechanisms, immune crosstalk, and therapeutic implications.Frontiers in immunology · 2026Review
- Natural compounds targeting glycolysis and TME in ovarian cancer: from metabolic crosstalk to therapeutic potential.Frontiers in pharmacology · 2026Review
- Herbal Composition Inhibits Mitochondrial Oxidative Phosphorylation to Prevent HER2-Positive Breast Cancer and Identifies Potential Active Compounds.International journal of molecular sciences · 2025Article
- Target identification of natural products in cancer with chemical proteomics and artificial intelligence approaches.Cancer biology & medicine · 2025Review
- Lactic acid metabolism: gynecological cancer's Achilles' heel.Discover oncology · 2025Review
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- Notch Signaling Suppression by Golden Phytochemicals: Potential for Cancer Therapy.Advanced pharmaceutical bulletin · 2024Review
- Phytotherapeutics in Cancer: From Potential Drug Candidates to Clinical Translation.Current topics in medicinal chemistry · 2024Review
- A comprehensive review on the potential of coumarin and related derivatives as multi-target therapeutic agents in the management of gynecological cancers.Frontiers in pharmacology · 2024Review
- Phenolic Acids-Mediated Regulation of Molecular Targets in Ovarian Cancer: Current Understanding and Future Perspectives.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Research progress on the mechanism of glycolysis in ovarian cancer.Frontiers in immunology · 2023Review
- Growth hormone remodels the 3D-structure of the mitochondria of inflammatory macrophages and promotes metabolic reprogramming.Frontiers in immunology · 2023Article
- Dicoumarol: from chemistry to antitumor benefits.Chinese medicine · 2022Review
- Recent advances in understanding the metabolic plasticity of ovarian cancer: A systematic review.Heliyon · 2022Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pyruvate dehydrogenase kinase 1 (PDK1) is overexpressed in ovarian cancer and thus is a promising anticancer therapeutic target. Our previous work suggests that coumarin compounds are potential inhibitors of PDKs. In this study, we used the ovarian cancer cell line SKOV3 as the model system and examined whether dicumarol (DIC), a coumarin compound, could inhibit ovarian cancer through targeting PDK1. We showed that DIC potently inhibited the kinase activity of PDK1, shifted the glucose metabolism from aerobic glycolysis to oxidative phosphorylation, generated a higher level of reactive oxygen species (ROS), attenuated the mitochondrial membrane potential (MMP), induced apoptosis, and reduced cell viability in vitro. The same phenotypes induced by DIC also were translated in vivo, leading to significant suppression of xenograft growth. This study not only identifies a novel inhibitor for PDK1, but it also reveals novel anticancer mechanisms of DIC and provides a promising anticancer therapy that targets the Warburg effect.
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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.