The resistance-nodulation-cell division family (RND) efflux pumps exemplify a unique phenomenon with drug resistance in different gram negative bacterial strains as a single mechanism causing resistance against several different classes of antibiotics. In Escherichia coli AG102 and Acinetobacter baumannii SBMox2 strains the well characterized RND efflux pumps are AcrAB-TolC and the AdeABC respe...

Multidrug resistance (MDR) is a severe obstacle to successful chemotherapy due to its complicated nature that involves multiple mechanisms, such as drug efflux by transporters (P-glycoprotein and breast cancer resistance protein, BCRP) and anti-apoptotic defense (B-cell lymphoma, Bcl-2). To synergistically and completely reverse MDR by simultaneous inhibition of pump and non-pump cellular resis...

The drug pump protein MRP2 is a membrane drug efflux transporter widely distributed in normal and tumor tissues. Its role is thought to be crucial for the disposition of many drugs and their substrates in different tissues. In this study, we aimed to examine the effects of systematic inflammation induced by lipopolysaccharide (LPS) on the expression and function of this transporter in rats. Jug...

Multidrug resistance membrane pumps reduce the efficacy of chemotherapies by exporting a wide panel structurally-divergent drugs. Here, to take advantage polyspecificity human Breast Cancer Resistance Protein (BCRP/ABCG2) and dimeric nature this pump, new indenoindole-based inhibitors from monomeric α,β-unsaturated ketone 4b phenolic derivative 5a were designed. A library 18 homo/hetero-dimers ...

Recently, multidrug-resistant pathogens have disseminated widely owing essentially to their increased multidrug efflux pump activity. Presently, there is a scarcity of new antibacterial agents, and hence, inhibitors of multidrug efflux pumps belonging to the resistance-nodulation-cell division (RND) family appear useful in the treatment of infections by multidrug-resistant pathogens. Moreover, ...

Isometric force and 45Ca efflux from the sarcoplasmic reticulum were measured at 19 degrees C in frog skeletal muscle fibers skinned by microdissection. After Ca2+ loading, application of the ionophores monensin, an Na+(K+)/H+ exchanger, or gramicidin D, an H+ greater than K+ greater than Na+ channel-former, evoked rapid force development and stimulated release of approximately 30% of the accum...

Isometric force and "Ca efflux from the sarcoplasmic reticulum were measured at 19°C in frog skeletal muscle fibers skinned by microdissection . After Ca" loading, application of the ionophores monensin, an Na+(K+)/ H' exchanger, or gramicidin D, an H+ > K' > Na' channel-former, evoked rapid force development and stimulated release of ^"30% of the accumulated "Ca within 1 min, whereas CCCP (car...

Moxifloxacin-resistant mutants of Brucella melitensis 16M [moxifloxacin minimum inhibitory concentration (MIC)=1mg/L] were selected in order to characterise fluoroquinolone resistance mechanisms in this species. Eight independent mutants were obtained, with moxifloxacin MICs of 16-32mg/L. The mutants displayed variable cross-resistance levels to other fluoroquinolone compounds, but no increased...

Lapatinib is a specific HER1 and 2 targeted tyrosine kinase inhibitor now widely used in combination with chemotherapy in the clinical setting. In this work, we investigated the interactions between lapatinib and specific chemotherapy agents (cisplatin, SN-38, topotecan) in a panel of cell lines [breast (n = 2), lung (n = 2), testis (n = 4)]. A high-sensitivity cell proliferation/cytotoxicity A...