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Characterization of the kinetics and mechanisms of inhibition of drugs interacting with the S.cerevisiae multidrug resistance pumps Pdr5p and Snq2p
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SYSNO ASEP 0327490 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Characterization of the kinetics and mechanisms of inhibition of drugs interacting with the S.cerevisiae multidrug resistance pumps Pdr5p and Snq2p Title Characterizace kinetiky a mechanismů inhibice u sloučenin interagujících s pumpami Pdr5p a Snq2p pro mnohočetnou látkovou resistenci u S.cerevisiae Author(s) Hendrych, T. (CZ)
Kodedová, M. (CZ)
Sigler, Karel (MBU-M) RID
Gášková, D. (CZ)Source Title Biochimica et biophysica acta - ISSN 0006-3002
Roč. 1788, č. 3 (2009), s. 717-723Number of pages 7 s. Language eng - English Country NL - Netherlands Keywords yeast MDR pump ; pump inhibitor ; membrane potential Subject RIV EE - Microbiology, Virology R&D Projects 1M0570 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z50200510 - MBU-M (2005-2011) UT WOS 000264271400016 DOI 10.1016/j.bbamem.2008.12.001 Annotation 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-C3(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-C3(3) by both pumps and confirmed the activation of membrane H+-ATPase by CCCP Workplace Institute of Microbiology Contact Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231 Year of Publishing 2010
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