National Repository of Grey Literature 2 records found  Search took 0.01 seconds. 
The influence of bosutinib, neratinib and ibrutinib inhibition on the activity of selected reductases from AKR and SDR superfamilies
Hudáčová, Lenka ; Wsól, Vladimír (advisor) ; Hofman, Jakub (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Lenka Hudáčová Supervisor: Ing. Vladimír Wsól, Ph.D. Title of diploma thesis: The influence of bosutinib, neratinib and ibrutinib inhibition on the activity of selected reductases from AKR and SDR superfamilies Anthracycline antibiotics (ANTs) are antineoplastic drugs. Daunorubicin (DAUN) is used in the treatment of acute leukaemia. Enzymes from aldo-keto reductase (AKR) and short-chain dehydrogenase/reductase (SDR) superfamilies mediate the reduction of DAUN to its C-13 alcohol metabolite daunorubicinol (DAUNOL), which is more cardiotoxic, less antineoplastic and is causing anthracycline resistance. In my diploma thesis, I examined the inhibitory effect of bosutnib, neratinib and imatinib on the activity of enzymes from the SDR and AKR superfamilies. The specific enzyme activity and inhibitory effect were estimated on the base of in vitro enzymatic production of DAUNOL by the ultra-high-performance liquid chromatography (UHPLC) system. MTT assay was used to measure DAUN and ibrutinib cytotoxicity effect on HCT116 cell culture. In vitro enzymatic activities for recombinant enzymes were decreased in order CBR1 > AKR1C3 > AKR1B1 > AKR1A1 > AKR7A2 > AKR1B10 > AKR1C1 > AKR1C2 > AKR1C4 > CBR3. The...
The influence of bosutinib, neratinib and ibrutinib inhibition on the activity of selected reductases from AKR and SDR superfamilies
Hudáčová, Lenka ; Wsól, Vladimír (advisor) ; Hofman, Jakub (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Lenka Hudáčová Supervisor: Ing. Vladimír Wsól, Ph.D. Title of diploma thesis: The influence of bosutinib, neratinib and ibrutinib inhibition on the activity of selected reductases from AKR and SDR superfamilies Anthracycline antibiotics (ANTs) are antineoplastic drugs. Daunorubicin (DAUN) is used in the treatment of acute leukaemia. Enzymes from aldo-keto reductase (AKR) and short-chain dehydrogenase/reductase (SDR) superfamilies mediate the reduction of DAUN to its C-13 alcohol metabolite daunorubicinol (DAUNOL), which is more cardiotoxic, less antineoplastic and is causing anthracycline resistance. In my diploma thesis, I examined the inhibitory effect of bosutnib, neratinib and imatinib on the activity of enzymes from the SDR and AKR superfamilies. The specific enzyme activity and inhibitory effect were estimated on the base of in vitro enzymatic production of DAUNOL by the ultra-high-performance liquid chromatography (UHPLC) system. MTT assay was used to measure DAUN and ibrutinib cytotoxicity effect on HCT116 cell culture. In vitro enzymatic activities for recombinant enzymes were decreased in order CBR1 > AKR1C3 > AKR1B1 > AKR1A1 > AKR7A2 > AKR1B10 > AKR1C1 > AKR1C2 > AKR1C4 > CBR3. The...

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