ArticleCancer biology & therapy2013
In vitro targeting of Polo-like kinase 1 in bladder carcinoma: comparative effects of four potent inhibitors.
Article in Cancer biology & therapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 36 citations in OpenAlex.
- The cell cycle regulator PLK1 promotes murine melanoma progression by regulating the transcription factor BACH1.PLoS biology · 2025Article
- GSK461364 Inhibits NLRP3 Inflammasome by Targeting NEK7 Phosphorylation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- A novel cuproptosis-related lncRNAs signature predicts prognostic and immune of bladder urothelial carcinoma.Frontiers in genetics · 2023Article
- An Overview of siRNA Delivery Strategies for Urological Cancers.Pharmaceutics · 2022Review
- Present and Future Perspective on PLK1 Inhibition in Cancer Treatment.Frontiers in oncology · 2022Review
- Resveratrol effects in bladder cancer: A mini review.Genetics and molecular biology · 2021Article
- Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1.Journal of medicinal chemistry · 2020Article
- Radiosensitization of Non-Small Cell Lung Cancer Cells by the Plk1 Inhibitor Volasertib Is Dependent on the p53 Status.Cancers · 2019Article
- In vitro study of the Polo-like kinase 1 inhibitor volasertib in non-small-cell lung cancer reveals a role for the tumor suppressor p53.Molecular oncology · 2019Article
- Pyroptosis in combinatorial treatment to improve cancer patients' outcome, is that what we want?EBioMedicine · 2019Article
- A PLK1 kinase inhibitor enhances the chemosensitivity of cisplatin by inducing pyroptosis in oesophageal squamous cell carcinoma.EBioMedicine · 2019Article
- The Emerging Role of Polo-Like Kinase 1 in Epithelial-Mesenchymal Transition and Tumor Metastasis.Cancers · 2017Review
- The GSK461364 PLK1 inhibitor exhibits strong antitumoral activity in preclinical neuroblastoma models.Oncotarget · 2017Article
- Plk1 Inhibitors in Cancer Therapy: From Laboratory to Clinics.Molecular cancer therapeutics · 2016Review
- Volasertib suppresses the growth of human hepatocellular carcinomaAmerican journal of cancer research · 2016Article
- Volasertib suppresses tumor growth and potentiates the activity of cisplatin in cervical cancer.American journal of cancer research · 2015Article
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Authors and funding
9 authors at 6 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Despite the improvements in neoadjuvant chemotherapy, the outcome of patients with advanced bladder cancer has changed very little over the past 30 years. In the present study we tested and compared the in vitro antitumor activities of four different inhibitors of Polo-like kinase 1 (PLK1) (BI 2536, BI 6727, GW843682X, and GSK461364), against 3 bladder carcinoma cell lines RT4, 5637 and T24. The impact on radiosensitivity and drug interactions in simultaneous treatments with cisplatin, methotrexate, and doxorubicin were also investigated. Our results showed that PLK1 inhibition prevented cell proliferation and clonogenicity, causing significant inhibition of invasion of tumor cells, though modest differences were observed between drugs. Moreover, all PLK1 inhibitors induced G 2/M arrest, with the subsequent induction of death in all 3 cell lines. Drug interactions studies showed auspicious results for all PLK1 inhibitors when combined with the commonly used cisplatin and methotrexate, though combinations with doxorubicin showed mostly antagonistic effects. Comparably, the four PLK1 inhibitors efficiently sensitized cells to ionizing radiation. Our findings demonstrate that irrespective of the inhibitor used, the pharmacological inhibition of PLK1 constrains bladder cancer growth and dissemination, providing new opportunities for future therapeutic intervention. However, further laboratorial and pre-clinical tests are still needed to corroborate the usefulness of using them in combination with other commonly used chemotherapeutic drugs.
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