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Inhibition of Na(+)/K(+)-ATPase by 5,6,7,8-tetrafluoro-3-hydroxy-2-phenylquinolin-4(1H)-one
J. Šeflová, P. Čechová, M. Biler, P. Hradil, M. Kubala,
Jazyk angličtina Země Francie
Typ dokumentu časopisecké články
- MeSH
- chinolony chemie farmakologie MeSH
- inhibitory enzymů chemie farmakologie MeSH
- prasata metabolismus MeSH
- simulace molekulového dockingu * MeSH
- sodíko-draslíková ATPasa antagonisté a inhibitory chemie metabolismus MeSH
- terciární struktura proteinů MeSH
- vazebná místa MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
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 favourable TFHPQ binding site for the K(+)-bound NKA, which is located in the proximity of the cytoplasmic C-terminus.
Dept of Organic Chemistry Faculty of Science Palacký University Olomouc Czech Republic
INSERM UMR 850 Univ Limoges School of Pharmacy Limoges France
Citace poskytuje Crossref.org
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- $a Šeflová, Jaroslava $u Dept. of Biophysics, Centre of Region Haná for Biotechnological and Agricultural Research, Faculty of Science, Palacký University, Olomouc-Holice, Šlechtitelů 27, Czech Republic. Electronic address: seflova.jaroslava@gmail.com.
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- $a 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 favourable TFHPQ binding site for the K(+)-bound NKA, which is located in the proximity of the cytoplasmic C-terminus.
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- $a Čechová, Petra $u Dept. of Biophysics, Centre of Region Haná for Biotechnological and Agricultural Research, Faculty of Science, Palacký University, Olomouc-Holice, Šlechtitelů 27, Czech Republic.
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- $a Biler, Michal $u Dept. of Biophysics, Centre of Region Haná for Biotechnological and Agricultural Research, Faculty of Science, Palacký University, Olomouc-Holice, Šlechtitelů 27, Czech Republic; INSERM UMR 850, Univ. Limoges, School of Pharmacy, Limoges, France.
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- $a Hradil, Pavel $u Dept. of Organic Chemistry, Faculty of Science, Palacký University, Olomouc, Czech Republic.
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- $a Kubala, Martin $u Dept. of Biophysics, Centre of Region Haná for Biotechnological and Agricultural Research, Faculty of Science, Palacký University, Olomouc-Holice, Šlechtitelů 27, Czech Republic. Electronic address: martin.kubala@upol.cz.
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