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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Brincat JP,Broccatelli F,Sabatini S,Frosini M,Neri A,Kaatz GW,Cruciani G,Carosati Edoi
10.1021/ml200293csubject
Has Abstractpub_date
2012-01-23 00:00:00pages
248-51issue
3issn
1948-5875journal_volume
3pub_type
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