Reference: Conseil G, et al. (2003) Potent competitive inhibition of drug binding to the Saccharomyces cerevisiae ABC exporter Pdr5p by the hydrophobic estradiol-derivative RU49953. Biochim Biophys Acta 1614(2):131-4

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Abstract


The hydrophobic estradiol-derivative RU49953 inhibits the energy-dependent interaction of yeast multidrug-transporter Pdr5p with its fluorescent drug-substrate rhodamine 6G. The potent inhibition is competitive towards drug binding (Ki=23+/-6 nM), whereas nucleoside-triphosphate hydrolysis is two-orders-of-magnitude less sensitive. RU49953 constitutes the most efficient inhibitor of drug binding to a yeast multidrug ABC exporter reported so far.

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Journal Article | Research Support, Non-U.S. Gov't
Authors
Conseil G, Perez-Victoria JM, Renoir JM, Goffeau A, Di Pietro A
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