Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein andS. aureusNorA
ACS Medicinal Chemistry Letters2012Vol. 3(3), pp. 248–251
Citations Over TimeTop 21% of 2012 papers
Jean Pierre Brincat, Fabio Broccatelli, Stefano Sabatini, Maria Frosini, Annalisa Neri, Glenn W. Kaatz, Gabriele Cruciani, Emanuele Carosati
Abstract
Thirty-two diverse compounds were evaluated for their ability to inhibit both Pgp-mediated efflux in mouse T-lymphoma L5178 MDR1 and NorA-mediated efflux in S. aureus SA-1199B. Only four compounds were strong inhibitors of both efflux pumps. Three compounds were found to inhibit Pgp exclusively and strongly, while seven compounds inhibited only NorA. These results demonstrate that Pgp and NorA inhibitors do not necessarily overlap, opening the way to safer therapeutic use of effective NorA inhibitors.
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