2024 Bucher 2006 pgp atpase

Bucher 2006 pgp atpase

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WebJun 1, 1995 · 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 basal ATPase activity (1.65 mumol/min per mg protein in the absence of added drugs or lipids) with an apparent Km for ATP of 0.4 mM. 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.

Structure-activity relationship studies of propafenone analogs …

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 … WebJul 19, 1994 · Pgp expressed in cultured Sf9 insect cells has been shown to exhibit a high capacity ATPase activity in the presence of a variety of drugs known to be transported by the Pgp (Sarkadi et al., J Biol Chem 267: 4854-4858, 1992). green giant peas with pearl onions

Analysis of the relationship between P-glycoprotein and …

WebJun 4, 2002 · Abstract. Extracellular acidification rates (ECARs) in response to eight different drugs activating or inhibiting the ATPase of P-glycoprotein (Pgp) were measured in real time by means of a Cytosensor microphysiometer in MDR1-transfected and corresponding wild-type cell lines, i.e., pig kidney cells (LLC-MDR1 and LLC-PK1) and mouse embryo ... WebJun 25, 2002 · Extracellular acidification rates (ECARs) in response to eight different drugs activating or inhibiting the ATPase of P-glycoprotein (Pgp) were measured in real time by means of a Cytosensor microphysiometer in MDR1-transfected and corresponding wild-type cell lines, i.e., pig kidney cells (LLC-MDR1 … WebATPase activity associated with P-glycoprotein (Pgp) is characterized by three drug-dependent phases: basal (no drug), drug-activated, and drug-inhibited. To under-stand the communication between drug-binding sites and ATP hydrolytic sites, we performed steady-state thermodynamic analyses of ATP hydrolysis in the pres- green giant peas in butter sauce

(PDF) Lipid environment determines the drug-stimulated ATPase …

Structure-activity relationship studies of propafenone …

WebMay 12, 2011 · TMP inhibits the efflux of Dox in MCF-7/dox cells and stimulates Pgp ATPase activity. a MCF-7/dox cells were treated with DOX (10 μM) and VRP (10 μM) or TMP at the indicated concentration for 3 h, then the cells were washed and incubated in fresh medium for the indicated time and the Dox concentration was determined. b … WebThe Pgp-ATPase activity was around 1.3 p..mol ATP hydro lyzed/min/mg membrane protein. Underthe assayconditions described, the plasma membranes (which are prepared in 0.25 Msucrose-contain ing buffer) are osmotically disrupted (Al-Shawi and Senior, 1993). green giant organic riced veggiesWebDec 1, 1997 · Pgp is an atypical translocating ATPase, with low affinity for ATP and high constitutive ATPase activity. Pgp also has an unusually broad specificity for hydrophobic substrates, including many chemotherapeutic drugs. flush valve seat repair kit

"WebIt 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 … " - Bucher 2006 pgp atpase

Bucher 2006 pgp atpase

Structure-activity relationship studies of propafenone …

WebAbstract. The anesthetics benzyl alcohol and the nonaromatic chloroform and diethyl ether, abolish P-glycoprotein (Pgp) ATPase activity in a mode that does not fit classical competitive, noncompetitive, or uncompetitive inhibition. At concentrations similar to those required for inhibition of ATPase activity, these anesthetics fluidize ... WebJan 4, 2008 · The Pgp–ATPase activation method has been used for screening Pgp interacting drugs (Polli et al., 2001) and also for determining kinetic parameters (Adachi et al., 2001, Xia et al., 2006). However, the kinetic parameters obtained with the Pgp–ATPase method varies between laboratories.

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WebThe effect of various inhibitors on partially purified Ha-Pgp showed that orthovanadate is a potent inhibitor of its ATPase activity, inhibiting it by 90% at a concentration of 2 mmol/L. Other inhibitors, such as EDTA, sodium azide, and molybdate resulted in only a 20% decrease in activity.

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 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), …

WebThese findings indicate a direct relationship between Pgp and abamectin resistance, and abamectin-induced Pgp expression may be involved in the modulation of abamectin efflux in T. cinnabarinus. Keywords: ATPase activity; Abamectin resistance; Gene expression; P-glycoprotein; Tetranychus cinnabarinus. 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.

WebOur 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.

WebFeb 23, 2024 · PGP, also known as multidrug resistance protein 1 (MDR1) or ATP-binding cassette sub-family B member 1 (ABCB1), is an ATP-dependent 170 kDa transmembrane protein that expels a variety of intracellular compounds from tissues for excretion. green giant peas and pearl onionsWebFeb 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. flush valves for drip irrigationWebFeb 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. flush valve seal mansfield 160WebNov 1, 2001 · P-glycoprotein (Pgp) affects the absorption, distribution, and clearance of a variety of compounds. Thus, identification of compounds that are Pgp substrates can aid drug candidate selection and optimization. Our goal was to evaluate three assays used to determine whether compounds are Pgp substrates. green giant rice cauliflowerWebMar 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, … green giant riced cauliflower asianWebSep 28, 2006 · Several lines of evidence suggest that gomisin A alters Pgp-substrate interaction but itself is neither a Pgp substrate nor competitive inhibitor. (1) First unlike Pgp substrates gomisin A inhibited the basal Pgp-associated ATPase (Pgp-ATPase) activity. flush valve stop capWebThe 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 … green giant riced broccoli