Potent competitive inhibition of drug binding to the Saccharomyces cerevisiae ABC exporter Pdr5p by the hydrophobic estradiol-derivative RU49953.

Conseil, Gwenaëlle;Perez-Victoria, José M;Renoir, J Michel;Goffeau, André;Di Pietro, Attilio
(2003) Biochimica et Biophysica Acta : international journal of biochemistry and biophysics — Vol. 1614, n° 2, p. 131-134 (2003)

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  • Conseil, Gwenaëlle
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  • Perez-Victoria, José M
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  • Renoir, J Michel
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  • Goffeau, AndréUCLouvain
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  • Di Pietro, Attilio
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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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Conseil, G., Perez-Victoria, J. M., Renoir, J. M., Goffeau, A., & Di Pietro, A. (2003). Potent competitive inhibition of drug binding to the Saccharomyces cerevisiae ABC exporter Pdr5p by the hydrophobic estradiol-derivative RU49953. Biochimica et Biophysica Acta : international journal of biochemistry and biophysics, 1614(2), 131-134. https://hdl.handle.net/2078.5/73253 (Original work published 2003)