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Targeting Casein Kinase 1 (CK1) in Hematological Cancers

Department of Experimental Biology, Faculty of Science, Masaryk University, 62500 Brno, Czech Republic
TG Therapeutics, New York, NY 10014, USA
Department of Cytokinetics, Institute of Biophysics, Academy of Sciences of the Czech Republic, 61265 Brno, Czech Republic
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(23), 9026;
Received: 24 October 2020 / Revised: 20 November 2020 / Accepted: 21 November 2020 / Published: 27 November 2020
(This article belongs to the Special Issue Protein Kinases: Function, Substrates, and Implication in Diseases)
The casein kinase 1 enzymes (CK1) form a family of serine/threonine kinases with seven CK1 isoforms identified in humans. The most important substrates of CK1 kinases are proteins that act in the regulatory nodes essential for tumorigenesis of hematological malignancies. Among those, the most important are the functions of CK1s in the regulation of Wnt pathways, cell proliferation, apoptosis and autophagy. In this review we summarize the recent developments in the understanding of biology and therapeutic potential of the inhibition of CK1 isoforms in the pathogenesis of chronic lymphocytic leukemia (CLL), other non-Hodgkin lymphomas (NHL), myelodysplastic syndrome (MDS), acute myeloid leukemia (AML) and multiple myeloma (MM). CK1δ/ε inhibitors block CLL development in preclinical models via inhibition of WNT-5A/ROR1-driven non-canonical Wnt pathway. While no selective CK1 inhibitors have reached clinical stage to date, one dual PI3Kδ and CK1ε inhibitor, umbralisib, is currently in clinical trials for CLL and NHL patients. In MDS, AML and MM, inhibition of CK1α, acting via activation of p53 pathway, showed promising preclinical activities and the first CK1α inhibitor has now entered the clinical trials. View Full-Text
Keywords: casein kinase 1; CK1α; CK1ε; leukemia; CLL; AML; MM; inhibitors; umbralisib; WNT pathway casein kinase 1; CK1α; CK1ε; leukemia; CLL; AML; MM; inhibitors; umbralisib; WNT pathway
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MDPI and ACS Style

Janovská, P.; Normant, E.; Miskin, H.; Bryja, V. Targeting Casein Kinase 1 (CK1) in Hematological Cancers. Int. J. Mol. Sci. 2020, 21, 9026.

AMA Style

Janovská P, Normant E, Miskin H, Bryja V. Targeting Casein Kinase 1 (CK1) in Hematological Cancers. International Journal of Molecular Sciences. 2020; 21(23):9026.

Chicago/Turabian Style

Janovská, Pavlína, Emmanuel Normant, Hari Miskin, and Vítězslav Bryja. 2020. "Targeting Casein Kinase 1 (CK1) in Hematological Cancers" International Journal of Molecular Sciences 21, no. 23: 9026.

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