Biochemical and Biophysical Research Communications
Regular ArticleAbsence of Cooperativity for MgATP and Verapamil Effects on the ATPase Activity of P-Glycoprotein Containing Membrane Vesicles
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Exploiting the metabolic energy demands of drug efflux pumps provides a strategy to overcome multidrug resistance in cancer
2021, Biochimica et Biophysica Acta - General SubjectsCitation Excerpt :Elevated glycolytic capacity has also been observed in P-gp expressing NCI-H460/R non-small cell lung carcinoma cells [30] and maintaining this activity was attributed to higher expression of enolase in resistant leukaemia cells [31]. Surprisingly, addition of the P-gp modulator verapamil did not further increase the rate of glycolysis in either MCF7/DX or NCI/ADRRES cells (Fig. 1d), despite its ability to markedly stimulate ATP hydrolysis by P-gp [32,33]. This may indicate that glycolysis was running at a near maximal capacity in the resistant cells at a rate that more than compensates for the ATP demands required for the basal activity of P-gp.
Role of P-glycoprotein inhibitors in ceramide-based therapeutics for treatment of cancer
2017, Biochemical PharmacologyCitation Excerpt :This interesting action well complements the long, enduring history of tamoxifen as a first generation P-gp inhibitor and modulator of multidrug resistance in cancer; tamoxifen interacts directly with P-gp but itself is not a substrate transport [26,27]. Although tamoxifen and desmethyltamoxifen (DMT) have been shown effective in combination with C6-cermide in acute myeloid leukemia (AML) [28,29], herein our aim was to discover alternatives to tamoxifen that would be void in antiestrogen activities. Additionally, having effective alternatives to tamoxifen would broaden the utility of ceramide as a cancer therapeutic.
Characterization of 3-methoxy flavones for their interaction with ABCG2 as suggested by ATPase activity
2014, Biochimica et Biophysica Acta - BiomembranesThe elimination of P-glycoprotein over-expressing cancer cells by antimicrobial cationic peptide NK-2: The unique way of multi-drug resistance modulation
2013, Experimental Cell ResearchCitation Excerpt :We assume that the difference between TQ's and Dex-VER's impacts on NK-2 activity is the consequence of their different mode of P-gp inhibition. Since Dex-VER stimulates P-gp ATPase activity behaving at the same time as the pump substrate [53], it is possible that it disturbs the transport of ions as well as the NK-2 binding next to P-gp. As for the TQ, which blocks P-gp ATPase activity [54] the suppression of P-gp transport accounts for reduced NK-2 effect.
Recognition of sulfonylurea receptor (ABCC8/9) ligands by the multidrug resistance transporter P-glycoprotein (ABCB1): Functional similarities based on common structural features between two multispecific ABC proteins
2011, Journal of Biological ChemistryCitation Excerpt :Membrane protein concentrations were determined by the Bradford method. In vesicles prepared from DC-3F/ADX, P-glycoprotein accounts for about 12–15% of total membrane proteins, whereas P-gp cannot be detected in the control vesicles prepared from the DC-3F cells (23). Experiments were performed using DC-3F cells as a control and DC-3F/ADX cells as a P-gp test.
Multidrug resistance protein 1 is not associated to detergent-resistant membranes
2007, Biochemical and Biophysical Research CommunicationsCitation Excerpt :Moreover, the expression level of a protein can also influence its DRM localization. As previously demonstrated, the lower the Pgp expression level, the higher the Pgp fraction located in the low-density DRMs [20,21]. To eliminate artefacts related to the protocol of DRMs extraction, we carried out confocal microscopy experiments that confirmed the absence of MRP1 in DRM structures.