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These results indicate that nilotinib reverses P-gp- mediated MDR by blocking the efflux function and potentiates DOX-induced cardiotoxicity.
Overall, our results indicate that nilotinib could reverse ABCB1- and ABCG2-mediated MDR by blocking the efflux function of these transporters.
Consistent with the cytotoxicity data, the drug accumulation results (Figure 1A) indicated that vardenafil significantly enhances intracellular paclitaxel accumulation by blocking the efflux of [3H]-paclitaxel in KB-C2 cells that overexpress ABCB1 (Figure 1A and 2B).
E2F1 downregulation has been shown to reverse this form of drug resistance by blocking the efflux pump [ 9].
These constituents might act by blocking the efflux pumps located in the cell membrane in the tested bacteria, preventing the extrusion of antibiotics in the cytoplasm and therefore restoring their activity as observed in this study [ 55, 56].
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Collectively, these findings highlighted WHI-P154 could significantly reverse ABCG2-mediated multidrug drug resistance by directly blocking the efflux function.
These TKIs can inhibit or reverse MDR by directly blocking the efflux of ABC transporter substrates, and they play a crucial role in overcoming chemotherapy resistance.
Similar to Nalp3 inflammasome activation by other particulate stimuli such as MSU or asbestos, hemozoin-induced IL-1β production was inhibited by blocking the K+ efflux from the cell by using the ATP-sensitive potassium channel inhibitor glybenclamide (Figure 2a,b and Figure 5b).
In HEK293-MRP7 cells, the reversal of MRP7-mediated MDR could be achieved by either decreasing MRP7 expression or blocking the efflux function of the transporter.
In other tumor cell models, cellular stress caused MRP1 and P-gp overexpression leading to increased Gemcitabine sensitivity, which could be abolished by blocking these efflux pumps with verapramil [ 31].
We have previously demonstrated that the efflux pump inhibitor phenylalanine-arginine ß-naphthylamide (PAßN) is able to block the efflux involved in chloramphenicol resistance in E. aerogenes clinical strains [13], [24].
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by blocking the egress
by blocking the release
by blocking the association
by blocking the formation
by blocking the interaction
by blocking the ability
by blocking the effect
by blocking the electron
by blocking the activity
by blocking the access
by blocking the degradation
by blocking the synthesis
by blocking the translation
by blocking the binding
by blocking the production
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