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PreadyPort BCRP and MDR1-Literature

PreadyPort BCRP and MDR1 in the Literature

  • A study that employed in vitro models of transporter-overexpressing MDCKII cells and Caco-2 monolayers along with an in vivo pharmacokinetic assay in male Wistar rats to (i) verify the inhibitory effect of rilpivirine to MDR1, BCRP, MRP2, OCT1, OCT2, or MATE1 transporters and to (ii) investigate possible ABC and/or SLC transporter-mediated interactions between rilpivirine and abacavir or lamivudine. More Info >>>>
  • Dei S, Braconi L, Romanelli MN, Teodori E. Recent advances in the search of BCRP- and dual P-gp/BCRP-based multidrug resistance modulators. Cancer Drug Resist 2019;2:710-743. More Info >>>
  • Atrasentan profoundly induced several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It was a moderate P-gp inhibitor (IC50 in P388/dx cells = 15.1 ± 1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells = 59.8 ± 11 μM). BCRP or P-gp overexpressing cells were slightly more resistant towards antiproliferative effects of atrasentan. More Info >>>
  • The Impact of Endogenous Breast Cancer Resistance Protein on Human P-Glycoprotein-Mediated Transport Assays Using LLC-PK1 Cells Transfected With Human P-Glycoprotein. Miyamoto, R., et al. (2019). We investigated the impact of porcine breast cancer resistance protein (Bcrp) in P-gp-mediated transport assays in LLC-PK1 cells. Porcine Bcrp mRNA was detected in both LLC-PK1 wildtype (WT) and LLC-PK1-P-gp cells by quantitative RT-PCR. To investigate the activity and impact of porcine Bcrp, we conducted transport assays using 6 typical BCRP substrates in LLC-PK1 cells. More Info >>>
  • Evaluation of Drug Transport in MDCKII-Wild Type, MDCKII-MDR1, MDCKII-BCRP and Caco-2 Cell Lines. Mukkavilli, R., Jadhav, G., Vangala, S. (2017). We observed that quinidine, a substrate for MDR1 transporter, showed efflux ratio (Papp B-A/ Papp A-B) of 838 in MDCKII-MDR1 cells which plummeted to 14 in presence of verapamil, a known inhibitor of MDR1. With MDCKII-WT cells, Papp of quinidine dropped from 2 to 1, in the presence of verapamil. The very high efflux ratios of MDR1 and BCRP substrates in transfected MDCKII cells clearly demonstrate the potential usefulness of these models to provide more definitive data to evaluate the transporter involvement compared to Caco-2 or MDCKII-WT cells. More Info >>>
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