A non-radioactive assay for precise determination of intracellular levels of imatinib and its main metabolite in Bcr-Abl positive cells

0368600 - ÚEB 2012 RIV NL eng J - Článek v odborném periodiku
Mlejnek, P. - Novák, Ondřej - Doležel, P.
A non-radioactive assay for precise determination of intracellular levels of imatinib and its main metabolite in Bcr-Abl positive cells.
Talanta. Roč. 83, č. 5 (2011), s. 1466-1471. ISSN 0039-9140. E-ISSN 1873-3573
Grant CEP: GA ČR GA301/08/1649
Výzkumný záměr: CEZ:AV0Z50380511
Klíčová slova: K562 cells * P-glycoprotein * Multidrug resistance * N-desmethyl imatinib * CGP 74588
Kód oboru RIV: EF - Botanika
Impakt faktor: 3.794, rok: 2011

Multidrug resistance (MDR) is often associated with overexpression of the P-glycoprotein (P-gp, ABCB1). It was demonstrated that the P-gp mediated efflux decreases the drug concentration in cancer cells which results in the failure of chemotherapy. However, the MDR phenotype in cancer cells obviously involves various mechanisms. Therefore, if we want to estimate a contribution of the P-gp expression to the MDR phenotype, a clear quantitative relationship between the intracellular drug level and cell sensitivity must be established. To achieve this goal, a sensitive and non-radioactive assay for precise determination of intracellular levels of imatinib and its main metabolite N-desmethyl imatinib (CGP 74588) has been developed.
Trvalý link: http://hdl.handle.net/11104/0202899