{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,30]],"date-time":"2026-09-30T18:00:15Z","timestamp":1790791215391,"version":"4.1.0"},"reference-count":144,"publisher":"MDPI AG","issue":"23","license":[{"start":{"date-parts":[[2020,11,27]],"date-time":"2020-11-27T00:00:00Z","timestamp":1606435200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001824","name":"Czech Science Foundation","doi-asserted-by":"publisher","award":["GX19-28347X"],"award-info":[{"award-number":["GX19-28347X"]}],"id":[{"id":"10.13039\/501100001824","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Ministry of Education, Youth and Sports of the CR","award":["CZ.02.1.01\/0.0\/0.0\/16_025\/0007381"],"award-info":[{"award-number":["CZ.02.1.01\/0.0\/0.0\/16_025\/0007381"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>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). CK1\u03b4\/\u03b5 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 PI3K\u03b4 and CK1\u03b5 inhibitor, umbralisib, is currently in clinical trials for CLL and NHL patients. In MDS, AML and MM, inhibition of CK1\u03b1, acting via activation of p53 pathway, showed promising preclinical activities and the first CK1\u03b1 inhibitor has now entered the clinical trials.<\/jats:p>","DOI":"10.3390\/ijms21239026","type":"journal-article","created":{"date-parts":[[2020,11,28]],"date-time":"2020-11-28T03:51:16Z","timestamp":1606535476000},"page":"9026","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":68,"title":["Targeting Casein Kinase 1 (CK1) in Hematological Cancers"],"prefix":"10.3390","volume":"21","author":[{"given":"Pavl\u00edna","family":"Janovsk\u00e1","sequence":"first","affiliation":[{"name":"Department of Experimental Biology, Faculty of Science, Masaryk University, 62500 Brno, Czech Republic"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0570-5072","authenticated-orcid":false,"given":"Emmanuel","family":"Normant","sequence":"additional","affiliation":[{"name":"TG Therapeutics, New York, NY 10014, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hari","family":"Miskin","sequence":"additional","affiliation":[{"name":"TG Therapeutics, New York, NY 10014, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9136-5085","authenticated-orcid":false,"given":"V\u00edt\u011bzslav","family":"Bryja","sequence":"additional","affiliation":[{"name":"Department of Experimental Biology, Faculty of Science, Masaryk University, 62500 Brno, Czech Republic"},{"name":"Department of Cytokinetics, Institute of Biophysics, Academy of Sciences of the Czech Republic, 61265 Brno, Czech Republic"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2020,11,27]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"414","DOI":"10.1016\/j.cbpa.2009.06.022","article-title":"The phosphoproteomics data explosion","volume":"13","author":"Lemeer","year":"2009","journal-title":"Curr. 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