Inhibitors of p-gp and bcrp
Webb15 apr. 2024 · MCF-7/ADR and MCF-7/MX100 cells incubated with P-gp and BCRP dual inhibitor candidates for 48 h were lysed and sonicated in RIPA buffer containing a … WebbML753286 is a potent, selective BCRP inhibitor with IC50 of 0.6 uM (BCRP efflux transporter), shows no activity against P-glycoprotein (P-gp), organic anion-transporting …
Inhibitors of p-gp and bcrp
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Webb1 jan. 2006 · Best studied thus far is elacridar, a highly efficient P-glycoprotein inhibitor that is an effective inhibitor of human BCRP and mouse BCRP1 that can be used … Webb8 feb. 2024 · P-glycoprotein (P-gp) and CYP3A4-interacting drugs influence plasma levels of non-vitamin K antagonist oral anticoagulants (NOACs). However, the clinical relevance is questioned. Therefore, the impact of pharmacokinetically-interacting drugs on the effectiveness and safety of NOACs in patients with atrial fibrillation (AF) was investigated.
Webb5 juni 2024 · Inhibitors of the P-gp drug efflux pump (also known as P-gp multidrug resistance transporter) listed above may increase serum concentrations of drugs that are substrates of P-gp, whereas inducers of P-gp drug efflux may decrease serum concentrations of substrates of P-gp. WebbImmunofluorescence, immunoprecipitation, MTT, flow cytometry and JC-1 staining analyses were conducted to study the reversal of MDR that is mediated by P-gp and BCRP in cancer cells. An ATPase assay and a structural analysis were also used to analyze the potential mechanisms by which BAY-1082439 specifically targets PI3K …
Webb16 apr. 2024 · The strongest inhibitor of P-gp and BCRP, which inhibited the transporters up to 80 to 90% compared to the respective positive controls, demonstrated the ability to reverse chemotherapy resistance in resistant cancer cell lines up to 5.6-fold. Webbför 9 timmar sedan · Determination of drug efflux, accumulation and topoisomerase I inhibition (months 18-36): The importance of critical residues in P-gp and BCRP efflux pumps, identified by in silico techniques, will be determined empirically by substituting them followed by measurement of drug efflux.
Webb1 apr. 2005 · To determine the effect of a P-gp and BCRP inhibitor on the brain penetration of imatinib, wild-type mice were treated with p.o. elacridar (100 mg/kg) 2 hours before an i.v. dose of [14 C]imatinib mesylate and compared with control wild-type mice (P < 0.05) and with control Bcrp1 knockout (P = 0.08) and control P-gp knockout mice (P = …
Webb1 juni 2024 · In this study, we assessed the BCRP-mediated efflux of several model drugs in Caco-2 cells using WK-X-34 as a dual inhibitor of P-glycoprotein (P-gp) and BCRP … rose charlyWebbTetrahydropalmatine (THP), with one chiral centre, is one of the major constituents of Rhizoma corydalis. THP is considered to possess analgesic, sedative, hypnotic actions … rose charging timeWebb1 dec. 2008 · An inhibitor of P-gp will increase thebioavailability of a P-gp substrate, whereasinduction of P-gp will reduce the bioavailabilityof a substrate drug. Digoxinis a drug that is a substrate of P-gp but isnot metabolized by CYP3A4. P-gp inhibitsits bioavailability and contributes toits renal and biliary secretion. rose charms for braceletsWebb16 sep. 2024 · PD0325901 is a weak substrate of P-gp and BCRP and reaches reasonable brain levels in wildtype mice. Of all five MEK inhibitors that were analyzed, PD0325901 was least efficiently transported in CETAs, although it still exhibited substrate affinity toward P-gp and BCRP (Figs. 4a and 4b, Table 1, Supporting Information storage units in pinebluff ncWebbof P-glycoprotein (P-gp) and BCRP and LY335979 as a selective inhibitor of P-gp. The permeability of daidzein was high with an apparent permeability coefficient for apical-to-basal transport (P AB) of 20.3 3 1026 cm/s. In addition, its efflux ratio (ER) was 1.55, indicating that the contribution of BCRP to its transport is minimal. storage units in pine bluff arWebb10 apr. 2024 · Iruplinalkib did not induce CYP1A2, CYP2B6 and CYP3A4 at therapeutic concentration, and was also a strong inhibitor of MATE1 and MATE2K transporters, as … storage units in phoenix oregonWebb24 aug. 2024 · h Inhibitor of P-gp (, defined as those increasing AUC or Cmax of digoxin, dabigatran, or edoxaban ≥1.5-fold). i Strong inhibitor of CYP3A4 and weak inducer of … storage units in piscataway