Kompletní analýza vlastností nových inhibitorů kasein kinázy 1 pro léčbu chronické lymfocytární leukémie


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Title in English Complete analysis of novel inhibitors of casein kinase 1 for the treatment of chronic lymphocytic leukemia

BRYJA Vítězslav JANOVSKÁ Pavlína PARUCH Kamil NĚMEC Václav GREGOROVÁ Michaela

Year of publication 2017
MU Faculty or unit

Faculty of Science

Description Research group of Assoc. Prof. Vítězslav Bryja (Faculty of Science MU) has shown that casein kinase 1 (CK1) plays an important role in the pathogenesis of chronic lymphocytic leukemia (CLL; Cancer Res., 2013, 73, 1491) and that inhibitors of CK1 show very promising results in the treatment of preclinical models of CLL. Subsequently, cooperation with Assoc. Prof. Kamil Paruch (Faculty of Science MU) has been established and his research group has prepared a number of new compounds with various substituent combinations around the central imidazole pharmacophore - the potential inhibitors of CK1. Analysis of the properties of these new compounds has shown that the selectivity of these compounds is better than those previously described in the literature and their efficacy against CLL is significantly higher than that of the current state-of-the-art CK1 inhibitor PF 670462.
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