ArticlePloS one2012
Effects of the CK2 inhibitors CX-4945 and CX-5011 on drug-resistant cells.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
27 citing papers in PubMed, 57 citations in OpenAlex.
- An Integrative Computational Pipeline for CK2 Inhibitor Discovery in Triple-Negative Breast Cancer Using Virtual Screening, Molecular Dynamics, Machine Learning, and Density Functional Theory.Pharmaceuticals (Basel, Switzerland) · 2026Article
- CK2 in the spotlight: decoding its role in hematological malignancies and therapeutic applications.Discover oncology · 2025Review
- Cancer selective cell death induction by a bivalent CK2 inhibitor targeting the ATP site and the allosteric αD pocket.iScience · 2024Article
- Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.ACS medicinal chemistry letters · 2023Article
- Inhibition of casein kinase 2 induces cell death in tyrosine kinase inhibitor resistant chronic myelogenous leukemia cells.PloS one · 2023Article
- A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action.RSC medicinal chemistry · 2022Article
- 4,5,7-Trisubstituted indeno[1,2-b]indole inhibits CK2 activity in tumor cells equivalent to CX-4945 and shows strong anti-migratory effects.FEBS open bio · 2022Article
- Mechanism of CK2 Inhibition by a Ruthenium-Based Polyoxometalate.Frontiers in molecular biosciences · 2022Article
- Targeting CK2 in cancer: a valuable strategy or a waste of time?Cell death discovery · 2021Review
- Development of a potent and selective chemical probe for the pleiotropic kinase CK2.Cell chemical biology · 2021Article
- Contribution of the CK2 Catalytic Isoforms α and α' to the Glycolytic Phenotype of Tumor Cells.Cells · 2021Article
- Role of CK2 inhibitor CX-4945 in anti-cancer combination therapy - potential clinical relevance.Cellular oncology (Dordrecht, Netherlands) · 2020Review
- Activated zinc transporter ZIP7 as an indicator of anti-hormone resistance in breast cancer.Metallomics : integrated biometal science · 2019Article
- Role of protein kinase CK2 in antitumor drug resistance.Journal of experimental & clinical cancer research : CR · 2019Review
- Knowledge-guided gene prioritization reveals new insights into the mechanisms of chemoresistance.Genome biology · 2017Article
- Exploring the Pivotal Role of the CK2 Hinge Region Sub-Pocket in Binding with Tricyclic Quinolone Analogues by Computational Analysis.Molecules (Basel, Switzerland) · 2017Article
- Targeting Protein Kinase CK2: Evaluating CX-4945 Potential for GL261 Glioblastoma Therapy in Immunocompetent Mice.Pharmaceuticals (Basel, Switzerland) · 2017Article
- Protein kinase CK2 modulates HSJ1 function through phosphorylation of the UIM2 domain.Human molecular genetics · 2017Article
- Specific inhibition of CK2α from an anchor outside the active site.Chemical science · 2016Article
- CK2α' Drives Lung Cancer Metastasis by Targeting BRMS1 Nuclear Export and Degradation.Cancer research · 2016Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
CK2 is a pleiotropic protein kinase, which regulates many survival pathways and plays a global anti-apoptotic function. It is highly expressed in tumor cells, and is presently considered a promising therapeutic target. Among the many inhibitors available for this kinase, the recently developed CX-4945 and CX-5011 have proved to be very potent, selective and effective in inducing cell death in tumor cells; CX-4945 has recently entered clinical trials. However, no data are available on the efficacy of these compounds to overcome drug resistance, a major reasons of cancer therapy failure. Here we address this point, by studying their effects in several tumor cell lines, each available as variant R resistant to drug-induced apoptosis, and normal-sensitive variant S. We found that the inhibition of endogenous CK2 was very similar in S and R treated cells, with more than 50% CK2 activity reduction at sub-micromolar concentrations of CX-4945 and CX-5011. A consequent apoptotic response was induced both in S and R variants of each pairs. Moreover, the combined treatment of CX-4945 plus vinblastine was able to sensitize to vinblastine R cells that are otherwise almost insensitive to this conventional antitumor drug. Consistently, doxorubicin accumulation in multidrug resistant (MDR) cells was greatly increased by CX-4945.In summary, we demonstrated that all the R variants are sensitive to CX-4945 and CX-5011; since some of the treated R lines express the extrusion pump Pgp, often responsible of the MDR phenotype, we can also conclude that the two inhibitors can successfully overcome the MDR phenomenon.
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Registered trials
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.