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@article{2262757,
author = {Němec, Václav and Khirsariya, PrashantKumar and Janovská, Pavlína and Martín Moyano, Paula and Maier, Lukáš and Procházková, Petra and Kebková, Pavlína and Gybeľ, Tomáš and Berger, BenedictandTilman and Chaikuad, Apirat and Reinecke, Maria and Kuster, Bernhard and Knapp, Stefan and Bryja, Vítězslav and Paruch, Kamil},
article_number = {11},
doi = {http://dx.doi.org/10.1002/anie.202217532},
keywords = {CK1; Chemical Probe; Inhibitor; Isoform Selectivity; Wnt Pathway},
language = {eng},
issn = {1433-7851},
journal = {Angewandte Chemie International Edition},
title = {Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity},
url = {https://doi.org/10.1002/anie.202217532},
volume = {62},
year = {2023}
}
TY - JOUR
ID - 2262757
AU - Němec, Václav - Khirsariya, PrashantKumar - Janovská, Pavlína - Martín Moyano, Paula - Maier, Lukáš - Procházková, Petra - Kebková, Pavlína - Gybeľ, Tomáš - Berger, Benedict-Tilman - Chaikuad, Apirat - Reinecke, Maria - Kuster, Bernhard - Knapp, Stefan - Bryja, Vítězslav - Paruch, Kamil
PY - 2023
TI - Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity
JF - Angewandte Chemie International Edition
VL - 62
IS - 11
SP - 1-7
EP - 1-7
PB - Wiley-VCH GmbH
SN - 14337851
KW - CK1
KW - Chemical Probe
KW - Inhibitor
KW - Isoform Selectivity
KW - Wnt Pathway
UR - https://doi.org/10.1002/anie.202217532
N2 - 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 MU1500 allow for specific targeting of CK1δ or dual inhibition of CK1δ/ϵ in cells. The compound MU1742 also efficiently inhibits CK1α and, to our knowledge, represents the first potent and highly selective inhibitor of this enzyme. In addition, we demonstrate that the central 1H-pyrrolo[2,3-b]pyridine-imidazole pharmacophore can be used as the basis of highly selective inhibitors of other therapeutically relevant protein kinases, e.g. p38α, as exemplified by the compound MU1299.
ER -
NĚMEC, Václav, PrashantKumar KHIRSARIYA, Pavlína JANOVSKÁ, Paula MARTÍN MOYANO, Lukáš MAIER, Petra PROCHÁZKOVÁ, Pavlína KEBKOVÁ, Tomáš GYBEĽ, Benedict-Tilman BERGER, Apirat CHAIKUAD, Maria REINECKE, Bernhard KUSTER, Stefan KNAPP, Vítězslav BRYJA a Kamil PARUCH. Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity. \textit{Angewandte Chemie International Edition}. Wiley-VCH GmbH, 2023, roč.~62, č.~11, s.~1-7. ISSN~1433-7851. Dostupné z: https://dx.doi.org/10.1002/anie.202217532.
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