Inhibition of Na+/K+-ATPase by 5,6,7,8-tetrafluoro-3-hydroxy-2-phenylquinolin-4(1H)-one

Publication date: Available online 20 April 2017
Source:Biochimie
Author(s): Jaroslava Šeflová, Petra Čechová, Michal Biler, Pavel Hradil, Martin Kubala
Na⁺/K⁺-ATPase (NKA) is an enzyme of crucial importance for all animal cells. We examined the inhibitory effects of halogenated phenylquinolinones on NKA. The 5,6,7,8-tetrafluoro-3-hydroxy-2-phenylquinolin-4(1H)-one (TFHPQ) was identified as an efficient NKA inhibitor with IC50 near 10 μM. The inhibition by TFHPQ is particularly efficient at higher concentrations of K⁺, where NKA adopts the E2 conformation. The experimental observations are in a good agreement with the outcomes from molecular docking. We identified an energetically favorable TFHPQ binding site for the K⁺-bound NKA, which is located in the proximity of the cytoplasmic C-terminus.



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