Ligand Promiscuity Between the Efflux Pumps Human P-Glycoprotein and S. Aureus NorA

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2014 Jun 6

PMID 24900460

Citations 4

Authors

Jean Pierre Brincat

Fabio Broccatelli

Stefano Sabatini

Maria Frosini

Annalisa Neri

Glenn W Kaatz

Gabriele Cruciani

Emanuele Carosati

Affiliations

Soon will be listed here.

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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