Zosuquidar (LY335979) is a widely used experimental P-glycoprotein (P-gp) inhibitor, which is commended as very potent but also as very specific for P-gp. In this in vitro and in silico study, we demonstrated for the first time that zosuquidar also inhibits organic cation transporters (OCT) 1-3, albeit less potently than P-gp. This still has to be kept in mind when zosuquidar is used to inhibit cellular efflux of P-gp substrates that are concurrently transported into the cells by OCTs. To avoid interference in these assays, zosuquidar concentrations should be kept below 1 µM.

• Klíčová slova
• LY335979, Metformin, Molecular docking, Organic cation transporters, P-glycoprotein, Zosuquidar,
• MeSH
• chinoliny * farmakologie   MeSH
• dibenzocyklohepteny MeSH
• HEK293 buňky MeSH
• lidé MeSH
• P-glykoprotein * antagonisté a inhibitory   MeSH
• proteiny přenášející organické kationty * antagonisté a inhibitory   metabolismus   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• chinoliny * MeSH
• dibenzocyklohepteny MeSH
• P-glykoprotein * MeSH
• proteiny přenášející organické kationty * MeSH
• zosuquidar trihydrochloride MeSH Prohlížeč