BACKGROUND The high mortality impact of infectious diseases will increase due to accelerated evolution of antibiotic resistance in important human pathogens. Development of antibiotic resistance is a evolutionary process inducing the erosion of the effectiveness of our arsenal of antibiotics. Resistance is not necessarily limited to a single class of antibacterial agents but may affect many unr...

Inhibition of drug efflux pumps such as P-glycoprotein represents a versatile approach for overcoming multidrug resistance in tumor therapy. Although numerous compounds have been identified as being able to inhibit P-glycoprotein, only little is known on the molecular basis of the drug–protein interaction. This article gives an overview of the different pharmacoinformatic approaches we used to ...

Reduced susceptibility to antimicrobials in Gram-negative bacteria may result from multiple resistance mechanisms, including increased efflux pump activity or reduced porin protein expression. Up-regulation of the efflux pump system is closely associated with multidrug resistance (MDR). To help investigate the role of efflux pumps on compound accumulation, a fluorescence-based assay was develop...

Moxifloxacin is a C8-methoxy (C8-OMe) fluoroquinolone that is highly active against Staphylococcus aureus, including many strains resistant to older fluoroquinolones such as ciprofloxacin. Available data indicate that it is a poor substrate for the NorA multidrug efflux pump. We produced a mutant of S. aureus in vitro (SA-K2068) with a novel non-NorA-mediated multidrug resistance phenotype char...

24 Among Acinetobacter spp., A. baumannii is the most frequently implicated in nosocomial 25 infections, in particular in intensive care units. It was initially thought that multidrug 26 resistance (MDR) in this species was mainly due to horizontal acquisition of resistance genes. 27 However, it has become recently obvious that increased expression of chromosomal genes for 28 efflux systems pla...

helicobacter hepaticus was discovered in 1992 as a cause of liver cancer in the a/jcr mouse model. in susceptible mice, infection by h. hepaticus causes chronic gastrointestinal inflammation leading to neoplasia. it can also cause morphological changes in breast-glands leading to neoplasm and adenocarcinoma in mouse models. studies performed on humans have revealed that h. hepaticus may also be...