ArticleMolecular and cellular biochemistry2015
Identification of a novel potent, selective and cell permeable inhibitor of protein kinase CK2 from the NIH/NCI Diversity Set Library.
Article in Molecular and cellular biochemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 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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Who cites it
17 citing papers in PubMed, 19 citations in OpenAlex.
- Discovery of 7,9-Dibromo-dihydrodibenzofuran as a Potent Casein Kinase 2 (CK2) Inhibitor: Synthesis, Biological Evaluation, and Structural Studies onACS pharmacology & translational science · 2024Article
- Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α.Journal of medicinal chemistry · 2020Article
- Identification and Biological Evaluation of CK2 Allosteric Fragments through Structure-Based Virtual Screening.Molecules (Basel, Switzerland) · 2020Article
- Protein Kinase CK2, a Potential Therapeutic Target in Carcinoma ManagementAsian Pacific journal of cancer prevention : APJCP · 2019Review
- Natural Compounds and Derivatives as Ser/Thr Protein Kinase Modulators and Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2019Review
- A facile consensus ranking approach enhances virtual screening robustness and identifies a cell-active DYRK1α inhibitor.Future medicinal chemistry · 2018Article
- Second-generation CK2α inhibitors targeting the αD pocket.Chemical science · 2018Article
- A π-Halogen Bond of Dibenzofuranones with the Gatekeeper Phe113 in Human Protein Kinase CK2 Leads to Potent Tight Binding Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2018Article
- Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structures with the Catalytic Subunit CK2α and Its Paralog CK2α'.Pharmaceuticals (Basel, Switzerland) · 2017Article
- Protein kinase CK2 regulates redox homeostasis through NF-κB and Bcl-xL in cardiomyoblasts.Molecular and cellular biochemistry · 2017Article
- CK2 in Cancer: Cellular and Biochemical Mechanisms and Potential Therapeutic Target.Pharmaceuticals (Basel, Switzerland) · 2017Review
- D11-Mediated Inhibition of Protein Kinase CK2 Impairs HIF-1α-Mediated Signaling in Human Glioblastoma Cells.Pharmaceuticals (Basel, Switzerland) · 2017Article
- The small-molecule kinase inhibitor D11 counteracts 17-AAG-mediated up-regulation of HSP70 in brain cancer cells.PloS one · 2017Article
- Specific inhibition of CK2α from an anchor outside the active site.Chemical science · 2016Article
- Protein Kinase CK2 Expression Predicts Relapse Survival in ERα Dependent Breast Cancer, and Modulates ERα Expression in Vitro.International journal of environmental research and public health · 2015Article
- The kinase inhibitor D11 induces caspase-mediated cell death in cancer cells resistant to chemotherapeutic treatment.Journal of experimental & clinical cancer research : CR · 2015Article
- Protein Kinase CK2: A Targetable BCR-ABL Partner in Philadelphia Positive Leukemias.Advances in hematology · 2015Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The anti-apoptotic protein kinase CK2 increasingly becomes an attractive target in cancer research with great therapeutic potential. Here, we have performed an in vitro screening of the Diversity Set III of the DTP program from the NCI/NIH, comprising 1600 compounds. We have identified 1,3-Dichloro-6-[(E)-((4-methoxyphenyl)imino)methyl] dibenzo(b,d) furan-2,7-diol (referred to as D11) to be a potent and selective inhibitor of protein kinase CK2. The D11 compound was tested against 354 eukaryotic protein kinases. By setting the threshold for inhibition to <2% remaining kinase activity, only DYRK1B, IRAK1 and PIM3 were inhibited to an extent as the tetrameric CK2 holoenzyme and its catalytic subunits α and α'. The IC50 values for the CK2α and CK2α' were on average 1-2 nM in comparison to the DYRK1B, IRAK1 and PIM3 kinases, which ranged from 18 to 49 nM. Cell permeability and efficacy of D11 were tested with cells in culture. In MIA PaCa-2 cells (human pancreatic carcinoma cell line), the phosphorylation of the CK2 biomarker CDC37 at S13 was almost completely inhibited in the presence of D11. This was observed both under normoxia and hypoxia. In the case of the human non-small cell lung carcinoma cell line, H1299, increasing amounts of D11 led to an inhibition of S380/T382/383 phosphorylation in PTEN, another biomarker for CK2 activity.
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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.