Characterization of the kinetics and mechanisms of inhibition of drugs interacting with the S. cerevisiae multidrug resistance pumps Pdr5p and Snq2p
Jazyk angličtina Země Nizozemsko Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem, validační studie
PubMed
19111673
DOI
10.1016/j.bbamem.2008.12.001
PII: S0005-2736(08)00395-7
Knihovny.cz E-zdroje
- MeSH
- ABC transportéry antagonisté a inhibitory chemie MeSH
- beta-alanin analogy a deriváty farmakologie MeSH
- fluorescenční spektrometrie MeSH
- karbocyaniny farmakologie MeSH
- karbonylkyanid-m-chlorfenylhydrazon farmakologie MeSH
- kinetika MeSH
- Saccharomyces cerevisiae - proteiny antagonisté a inhibitory chemie MeSH
- takrolimus farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- validační studie MeSH
- Názvy látek
- 3,3'-dipropylthiacarbocyanine MeSH Prohlížeč
- ABC transportéry MeSH
- beta-alanin MeSH
- karbocyaniny MeSH
- karbonylkyanid-m-chlorfenylhydrazon MeSH
- PDR5 protein, S cerevisiae MeSH Prohlížeč
- Saccharomyces cerevisiae - proteiny MeSH
- SNQ2 protein, S cerevisiae MeSH Prohlížeč
- takrolimus MeSH
- undecyl 3-(dimethylamino)propionate MeSH Prohlížeč
We have developed a novel screening method that measures the kinetics and potencies of inhibitors of the yeast multidrug resistance pumps Pdr5p and Snq2p. The assay uses the potentiometric fluorescent probe diS-C(3)(3) (as a benchmark substrate of both pumps) to distinguish drugs with minimal effects on plasma membrane potential as a marker of side-effects on membrane function and integrity. Using FK506, its structural analog rapamycin and enniatin B, we showed that our assay can also be used to determine the minimum drug concentration causing an immediate inhibitory effect and to compare the inhibitory potencies of the drug on the two pumps. We found that the protonophore CCCP effectively inhibits the transport of diS-C(3)(3) by both pumps and confirmed the activation of membrane H(+)-ATPase by CCCP.
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