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. ...
Several transporters appear to be important in transporting various drugs. Many patients, who receive morphine as analgesic medication, also receive other medications with potency of changing morphine transport by affecting P-glycoprotein (P-GP) and oatp2 transport system. This could influence morphine ...
High MRP-1 cell membrane protein expression might be useful to identify those patients that are most likely to benefit from more aggressive treatment, combination treatment with standard chemotherapeutics and MRP-1 inhibitors, or treatment with a non-MRP-1 substrate (Roundhill and Burchill, 2012)....
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...
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 ...
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 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 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...
Transportation by ATP-dependent efflux pumps such as P-glycoprotein (PGP), encoded by genes associated with multidrug resistance, is a well-known mechanism that allows cells to maintain substrate homeostasis but also to evade drug therapy [30,31]. PGP plays a significant role in multidrug resistan...