Multidrug Efflux Pumps

OprM, the outer membrane component of the MexAB-OprM multidrug efflux pump ofPseudomonas aeruginosa, hasbeenassumed to facilitate the export of antibiotics across the outer membrane of this organism. Here we purified to homogeneity the OprM protein, reconstituted it into lipo-somemembranes, and tested its channel activitybyusing the liposome swellingassay. Itwas demonstrated thatOprMis a channel-forming protein and exhibits the channel property that amino acids diffuse more efficiently than saccharides....

8p research12 23-04-2013 40 4   Download

Multidrug resistance (MDR) in tumour cells is often caused by the overexpression of the plasma drug transporter P-glycoprotein (P-gp). This protein is an active efflux pump for chemotherapeutic drugs,natural products and hydro-phobicpeptides.Despite theadvancesof recent years,we still have an unclear view of the molecular mechanismby which P-gp transports such a wide diversity of compounds across themembrane.

10p tumor12 20-04-2013 42 4   Download

The drug concentration inside multidrug-resistant cells is the outcome of competition between the active export of drugs by drug efflux pumps, such as P-glycoprotein (Pgp), and the passive permeation of drugs across the plasma membrane. Thus, reversal of multidrug resistance (MDR) can occur either by inhibition of the efflux pumps or by acceleration of the drug per-meation.

11p media19 05-03-2013 29 4   Download

Human P-glycoprotein (P-gp), which conveys multidrug resistance, is an ATP-dependent drug efflux pump that transports a wide variety of struc-turally unrelated compounds out of cells. P-gp possesses a ‘linker region’ of75 amino acids that connects two homologous halves, each of which contain a transmembrane domain followed by a nucleotide-binding domain.

13p viettel02 22-02-2013 50 3   Download

One of the Holy Grails of ATP-binding cassette transporter research is a structural understanding of drug binding and transport in a eukaryotic multidrug resistance pump. These transporters are front-line mediators of drug resistance in cancers and represent an important therapeutic target in future chemotherapy.

14p mobifone23 18-01-2013 34 4   Download