About: 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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About: Characterization of the kinetics and mechanisms of inhibition of drugs interacting with the S.cerevisiae multidrug resistance pumps Pdr5p and Snq2p Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	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 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 (en)
Title	Characterization of the kinetics and mechanisms of inhibition of drugs interacting with the S.cerevisiae multidrug resistance pumps Pdr5p and Snq2p Characterization of the kinetics and mechanisms of inhibition of drugs interacting with the S.cerevisiae multidrug resistance pumps Pdr5p and Snq2p (en)
skos:prefLabel	Characterization of the kinetics and mechanisms of inhibition of drugs interacting with the S.cerevisiae multidrug resistance pumps Pdr5p and Snq2p Characterization of the kinetics and mechanisms of inhibition of drugs interacting with the S.cerevisiae multidrug resistance pumps Pdr5p and Snq2p (en)
skos:notation	RIV/61388971:_____/09:00327490!RIV10-MSM-61388971
http://linked.open...avai/riv/aktivita	P S Z
http://linked.open...avai/riv/aktivity	P(1M0570), S, Z(AV0Z50200510), Z(MSM0021620835)
http://linked.open...iv/cisloPeriodika	3
http://linked.open...vai/riv/dodaniDat	2010
http://linked.open...aciTvurceVysledku	Sigler, Karel
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Mikrobiologický ústav AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	306800
http://linked.open...ai/riv/idVysledku	RIV/61388971:_____/09:00327490
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	yeast MDR pump; pump inhibitor; membrane potential (en)
http://linked.open.../riv/klicoveSlovo	pump inhibitor yeast MDR pump membrane potential
http://linked.open...odStatuVydavatele	NL - Nizozemsko
http://linked.open...ontrolniKodProRIV	[6E43757EAB22]
http://linked.open...i/riv/nazevZdroje	Biochimica et biophysica acta
http://linked.open...in/vavai/riv/obor	EE
http://linked.open...ichTvurcuVysledku	1 (xsd:int)
http://linked.open...cetTvurcuVysledku	4 (xsd:int)
http://linked.open...vavai/riv/projekt	Research Centre for Study of Extract Compounds of Barley and Hop
http://linked.open...UplatneniVysledku	2009
http://linked.open...v/svazekPeriodika	1788
http://linked.open...iv/tvurceVysledku	Sigler, Karel Kodedová, M. Gášková, D. Hendrych, T.
http://linked.open...ain/vavai/riv/wos	000264271400016
http://linked.open...n/vavai/riv/zamer	Microorganisms in Research and Biotechnology Fyzika molekulárních, makromolekulárních a biologických systémů
issn	0006-3002
number of pages	7 (xsd:int)

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