Bucher 2006 pgp atpase
WebAbstract. The human multidrug resistance protein, or P-glycoprotein (Pgp), exhibits a high-capacity drug-dependent ATP hydrolytic activity that is a direct reflection of its drug transport capability. This activity is readily measured in membranes isolated from cultured insect cells infected with a baculovirus carrying the human mdr1 cDNA. WebThe area under the curves of Pgp-ATPase activity time (AUC (Activity 0-24)) following DOX administration in TAM-treated group was significantly lower than that of the control group, indicating an overall inhibitory effect of TAM on Pgp …
Bucher 2006 pgp atpase
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WebThe P-glycoprotein multidrug transporter (Pgp; ABCB1) is an ATP-binding cassette (ABC) protein that has been implicated in the multidrug resistance of human cancers. Pgp couples ATP hydrolysis to active extrusion from the cell of a broad array of amphipathic compounds via an ill-defined mechanism. WebThe main goal of this work was to investigate Pgp efflux pump activity and expression in T. cruzi lines submitted to in vitro induced resistance to the compounds 4-N-(2-methoxy styryl)-thiosemicarbazone (2-Meotio) and benznidazole (Bz) and to verify the stability of the resistant phenotypes during the parasite life cycle.
WebNov 1, 1999 · Propafenone analogs (PAs) were previously identified as potent inhibitors of P-glycoprotein (Pgp)-mediated toxin efflux. For this as well as other classes of Pgp inhibitors, lipophilicity as well as hydrogen bond acceptor strength are important determinants of biological activity. WebPurified P-glycoprotein ATPase from Helicoverpa armigera (Ha-Pgp), reconstituted in proteoliposomes composed of phospholipids and cholesterol, shows higher ATPase activity in the presence of cholesterol than in its absence. The Ha-Pgp ATPase activity was increased 30-40% with cholesterol.
WebFeb 1, 2024 · erapamil-induced stimulation of ATPase activity in DDM-E. coli lipid mixed micelles. Purified Pgp in detergent solution was activated with 1% E. coli polar lipids and 10 mM DTT as described in ... Web382 F. J. Sharom and others mycinA1andconcanamycinsAandB.Finally, the endogenous phospholipids associated with Pgp were identified and the phosphorylation status ofthe purified protein wasexplored.
WebP-glycoprotein (P-gp) is a transmembrane efflux transporter which possesses many important functions in drug absorption, disposition, metabolism, and toxicity. The ultimate goal of investigating drug interactions between P-gp and drug molecules in early drug discovery is to understand the contributi …
WebThe purpose of this study was to investigate the possible interaction of P-gp with each of four major marijuana constituents: Delta (9)-tetrahydrocannabinol (THC), 11-nor-Delta (9)-tetrahydrocannabinol-carboxylic acid (THC-COOH), cannabinol (CBN), … haus custom cabinetsWebIt can be concluded that Pgp is a constitutively active, adenine nucleotide-specific ATPase whose catalytic activity can be modulated by both drugs and phospholipids. P-Glycoprotein (Pgp) was isolated from CHRC5 membranes by selective detergent extraction and further purified by lentil lectin affinity chromatography. The purified product displayed a very high … borderlands 3 romanceWebFeb 9, 1996 · The aim of the present study was to demonstrate that the modulation of P-glycoprotein (Pgp) ATPase activity by peptides, drugs, and chemosensitizers takes place on a common drug pharmacophore. To this end, a highly emetine-resistant Chinese hamster ovary cell line was established, in which Pgp constituted 18% of plasma membrane protein. borderlands 3 ring the bellWebMar 16, 2016 · The calcium channel blocker verapamil (Figure 1A), which is commonly used to control hypertension, chest pain and arrhythmia [15–19], functions as a substrate and an inhibitor of the transporter [].From results of in vitro studies, the drug is known to activate Pgp-coupled ATP-hydrolysis [].This drug manifests a spectrum of characteristics, … haus custom homesWebFeb 23, 2024 · We tested four different ratios of Bio-Beads of 1, 2, 3, and 4 mg per 1 mg of purified Pgp. 2 mg of Bio-Beads per 1 mg Pgp produced high ATPase activity while increasing the ratio of Bio-Beads to Pgp diminished the yield of Pgp-discs. haus curveWebOur goal was to evaluate three assays used to determine whether compounds are Pgp substrates. Sixty-six compounds were tested in monolayer efflux, ATPase, and calcein-AM assays. Assay results yielded two categories of compounds. Category I (n = 35) exhibited concordance across the assays. borderlands 3 robot characterWebThe methods included the use of 1) standard Pgp substrate rhodamine 123 to assay the Pgp efflux system in BBMEC, 2) luciferin/luciferase assay for ATP intracellular levels, and 3) 1,6-diphenyl-1,3,5-hexatriene for membrane microviscosity. borderlands 3 rowan call