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Information × Registration Number 0210U003840, 0107U004939 , R & D reports Title Optimization of the protein kinase СК2 inhibitors and evaluation of their biological activity on cancer cells. popup.stage_title Head Yarmoluk Sergii Mykolaiovych, Registration Date 17-03-2010 Organization Institute of Molecular Biology and Genetics of NASU popup.description2 The new inhibitors of protein kinase CK2 have been developed using molecular modeling methods, directed organic synthesis and in vitro tests. Binding mode for the flavone derivatives at ATP - binding site of CK2 was proposed. Chemical optimization of flavones was performed on the base of binding mode. The methods of synthesis were developed and the row of nanomolar inhibitors of CK2 has been obtained. Evaluation of the inhibitors on five protein kinases revealed considerable selectivity towards CK2. The developed inhibitors were investigated with cultured human embryonic astrocytes (HAST-40), glioma cell line (U87MG) and human brain microvascular cells. A striking effect of CK2 inhibitors on cell morphology was observed. Product Description popup.authors Бджола Володимир Григорович Голуб Андрій Григорович Кухаренко Олександр Петрович Лукашов Сергій Степанович Приходько Андрій Олександрович Сапелкін Владислав Миколайович popup.nrat_date 2020-04-02 Close