In addition to mediating or limiting the absorption, distribution, excretion, and toxicity of many drugs, P-gp is the potential locus of a number of pharmacokinetic drug-drug interactions when two drugs, one a substrate and the other a substrate or inhibitor of the transporter, are co-...
Includes: • 1 vial ATP Detection Substrate (lyophilized) • 10ml ATP Detection Buffer • 10ml Pgp-Glo™ Assay Buffer • 1ml 50mM MgATP • 100μl 10mM Verapamil • 250μl 10mM Na3VO4 (sodium orthovanadate) Storage Conditions: Store Recombinant Human Pgp Membranes at –70°C. ...
The protein encoded by this gene is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. This protein also ...
Baill.) sensitized Pgp-MDR HepG2-DR cells by interfering with the function of Pgp-substrate complexes. In Pgp-MDR cells, SCH enhanced the cytotoxicity of cancer drugs that are Pgp substrates and restored vinblastine-induced G 2/M arrest without lowering Pgp expression. SCH increased cellular ...
PGP–substrate drug pharmacokinetics and drug response, highlights methodological limitations of existing studies, including inadequate power, potential confounding by co-morbidity and co-medication, multiple testing, poor definition of disease phenotype and outcomes, and analysis of multiple drugs that might...
Feldmann M, Koepp M (2012) P-glycoprotein imaging in temporal lobe epilepsy: in vivo PET experiments with the Pgp substrate [11C]-verapamil. Epilepsia 53(Suppl. 6):60-63.Feldmann M, Koepp M. P-glycoprotein imaging in temporal lobe epilepsy: in vivo PET experiments with the Pgp ...
Furthermore, nilotinib produces a concentration-dependent inhibition of the ABCG2-mediated transport of [314]-methotrexate (MTX), as well as [31-1]-E217f3G, a physiological substrate of ABCG2. Uptake studies in membrane vesicles overexpressing ABCG2 have indicated that nilotinib inhibits ABCG2...
Furthermore, nilotinib produces a concentration-dependent inhibition of the ABCG2-mediated transport of methotrexate (MTX), as well as E 217尾G a physiological substrate of ABCG2. Uptake studies in membrane vesicles overexpressing ABCG2 have indicated that nilotinib inhibits ABCG2 similar to other...
Furthermore, nilotinib directly and potently interacts with ABCB1 and ABCG2 at its drug-binding site as shown by photo affinity labelling assay, where nilotinib competitively displaces [125I]-IAAP from its known substrate binding sites of these transporters. This direct interaction of nilotinib was...