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Titel:

Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity

Dokumenttyp:
Zeitschriftenaufsatz
Autor(en):
Němec, Václav; Khirsariya, Prashant; Janovská, Pavlína; Moyano, Paula Martín; Maier, Lukáš; Procházková, Petra; Kebková, Pavlína; Gybel', Tomáš; Berger, Benedict‐Tilman; Chaikuad, Apirat; Reinecke, Maria; Kuster, Bernhard; Knapp, Stefan; Bryja, Vítězslav; Paruch, Kamil
Abstract:
Casein kinases 1 (CK1) are key signaling molecules that have emerged recently as attractive therapeutic targets in particular for the treatment of hematological malignancies. Herein, we report the identification of a new class of potent and highly selective inhibitors of CK1α, δ and ϵ. Based on their optimal in vitro and in vivo profiles and their exclusive selectivity, MU1250, MU1500 and MU1742 were selected as quality chemical probes for those CK1 isoforms. At proper concentrations, MU1250 and...     »
Stichworte:
BayBioMS; CK1; Chemical Probe; Inhibitor; Isoform Selectivity; Wnt Pathway
Zeitschriftentitel:
Angewandte Chemie International Edition
Jahr:
2023
Volltext / DOI:
doi:10.1002/anie.202217532
Verlag / Institution:
Wiley
E-ISSN:
1433-78511521-3773
Publikationsdatum:
02.02.2023
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