Can P glycoprotein mediate resistance to nilotinib in human leukemia cells?

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F13%3A33145121" target="_blank" >RIV/61989592:15110/13:33145121 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S1043661812001995" target="_blank" >http://www.sciencedirect.com/science/article/pii/S1043661812001995</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.phrs.2012.10.012" target="_blank" >10.1016/j.phrs.2012.10.012</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Can P glycoprotein mediate resistance to nilotinib in human leukemia cells?

Popis výsledku v původním jazyce

The effect of P-glycoprotein (P-gp, ABCB1, MDR1) expression on cell resistance to nilotinib was studied in human leukaemia cells. We used K562/Dox cells overexpressing P-gp and their variants (subclones) with a gradually decreased P-gp expression. Thesesubclones were established by stable transfection of K562/Dox cells with a plasmid vector expressing shRNA targeting the ABCB1 gene. Functional analysis of P-gp using a specific fluorescent probe indicated gradually decreased dye efflux which was proportional to the P-gp expression. We observed that K562/Dox cells overexpressing P gp contained a significantly reduced intracellular level of nilotinib when compared to their counter partner K562 cells, which do not express P-gp. This effect was accompaniedby a decreased sensitivity of the K562/Dox cells to nilotinib. Importantly, cells with downregulated expression of P gp gradually lost their ability to decrease the intracellular level of nilotinib although they still significantly decre

Název v anglickém jazyce

Can P glycoprotein mediate resistance to nilotinib in human leukemia cells?

Popis výsledku anglicky

The effect of P-glycoprotein (P-gp, ABCB1, MDR1) expression on cell resistance to nilotinib was studied in human leukaemia cells. We used K562/Dox cells overexpressing P-gp and their variants (subclones) with a gradually decreased P-gp expression. Thesesubclones were established by stable transfection of K562/Dox cells with a plasmid vector expressing shRNA targeting the ABCB1 gene. Functional analysis of P-gp using a specific fluorescent probe indicated gradually decreased dye efflux which was proportional to the P-gp expression. We observed that K562/Dox cells overexpressing P gp contained a significantly reduced intracellular level of nilotinib when compared to their counter partner K562 cells, which do not express P-gp. This effect was accompaniedby a decreased sensitivity of the K562/Dox cells to nilotinib. Importantly, cells with downregulated expression of P gp gradually lost their ability to decrease the intracellular level of nilotinib although they still significantly decre

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

—

Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)<br>S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2013

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Pharmacological Research

ISSN

1043-6618

e-ISSN

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Svazek periodika

67

Číslo periodika v rámci svazku

1

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

5

Strana od-do

79-83

Kód UT WoS článku

000313767400009

EID výsledku v databázi Scopus

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