Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein and S. aureus NorA
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- 作者：Jean Pierre Brincat ; Fabio Broccatelli ; Stefano Sabatini ; Maria Frosini ; Annalisa Neri ; Glenn W. Kaatz ; Gabriele Cruciani ; Emanuele Carosati
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：March 8, 2012
- 年：2012
- 卷：3
- 期：3
- 页码：248-251
- 全文大小：223K
- 年卷期：v.3,no.3(March 8, 2012)
- ISSN：1948-5875
文摘
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.