New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights
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Summary
The identification and characterization of 2,8‐difurandicarboxylic acid derivatives as a new class of nanomolar ATP‐competitive inhibitors of CK2 and Pim kinases are reported, highlighting that 2 functionally related kinases from different kinome branches display exquisite sensitivity to a common inhibitor.
- Type
- article
- Published
- 2010-09-01
- Cited by
- 61
- References
- 90
- OpenAlex
- https://openalex.org/W2160953463
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:40621379
Keywords
Kinome, Kinase, Threonine, Biochemistry, Casein kinase 1
References
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- Sur quelques modifications d'activité biologique consécutives à l'accolement d'un second cycle nitrofuranne à l'homocycle de nitroarénofurannes
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- The Replacement of ATP by the Competitive Inhibitor Emodin Induces Conformational Modifications in the Catalytic Site of Protein Kinase CK2*
- Heat-induced Relocalization of Protein Kinase CK2
- Automatic processing of rotation diffraction data from crystals of initially unknown symmetry and cell constants
- The CCP4 suite: programs for protein crystallography.
- The 44 kDa Pim-1 kinase directly interacts with tyrosine kinase Etk/BMX and protects human prostate cancer cells from apoptosis induced by chemotherapeutic drugs
- Targeting CK2 for cancer therapy.
- Nuclear localization of protein kinase CK2 catalytic subunit (CK2alpha) is associated with poor prognostic factors in human prostate cancer.
- The selectivity of inhibitors of protein kinase CK2: an update.
- Role for casein kinase 2 in the regulation of HIF‐1 activity
- Expanding the chemical diversity of CK2 inhibitors
- Casein kinase 2 inhibition decreases hypoxia-inducible factor-1 activity under hypoxia through elevated p53 protein level
Cited by
- Cell-permeable dual inhibitors of protein kinases CK2 and PIM-1: structural features and pharmacological potential
- [Strength and specificity of the CMBA screening platform for bioactive molecules discovery].
- In vivo elucidation of PIM kinase role in tumourigenesis
- Exploiting the repertoire of CK2 inhibitors to target DYRK and PIM kinases.
- PIM1 kinase as a target for cancer therapy
- Inhibition of Pim1 kinase activation attenuates allergen-induced airway hyperresponsiveness and inflammation.
- PIM1 kinase inhibitors induce radiosensitization in non-small cell lung cancer cells.
- Crystal Structure of Pim1 Kinase in Complex with a Pyrido[4,3-D]Pyrimidine Derivative Suggests a Unique Binding Mode
- Low-density crystal packing of human protein kinase CK2 catalytic subunit in complex with resorufin or other ligands: a tool to study the unique hinge-region plasticity of the enzyme without packing bias.
- 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.
- Pharmacokinetic characterization of CK2 inhibitor CX-4945
- Antitumor activity of pyridocarbazole and benzopyridoindole derivatives that inhibit protein kinase CK2.
- Pim kinases in cancer: diagnostic, prognostic and treatment opportunities.
- Targeting Pim kinases for cancer treatment: opportunities and challenges.
- Flexibility of the P-loop of Pim-1 kinase: observation of a novel conformation induced by interaction with an inhibitor.
- High-Throughput Kinase Profiling: A More Efficient Approach towards the Discovery of New Kinase Inhibitors
- Structural and functional analysis of the flexible regions of the catalytic α-subunit of protein kinase CK2.
- Structural and functional determinants of protein kinase CK2α: facts and open questions
- Connexin 30 expression inhibits growth of human malignant gliomas but protects them against radiation therapy.
- Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells.
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