ABC Transporters and Cancer by Toshihisa Ishikawa, John Schuetz PDF
By Toshihisa Ishikawa, John Schuetz
ABC Transporters and Cancer offers important details at the interesting and fast-moving box of melanoma study. right here, striking and unique reports are awarded on a number of issues. This quantity covers ABC transporters and melanoma, and is appropriate for researchers and scholars alike.
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Additional resources for ABC Transporters and Cancer
Retrospective analysis of our data suggests that only at very high taxane plasma levels, which are obtained shortly after intravenous but not oral administration, ABCB1 plays a substantial role in limiting taxane brain accumulation. At lower plasma taxane concentrations, probably some other, as yet unidentified, transporter(s) dominate this process, obscuring any contribution of ABCB1 in the BBB. 5 Possible effects of ABCB1 inhibitors on enhancing taxane antitumor efficacy As illustrated above, safely boosting availability of orally administered taxanes with Abcb1a/1b inhibitors in mice is feasible.
The final review provides an overview of a widely used pyrimidine-based anticancer drug, 5-fluorouracil (5-FU), from a transporter perspective. Following uptake, 5-FU is anabolized to nucleosides then nucleotides. While there are well-known mechanisms of enzymatic resistance to 5-FU, the role of transporters in 5-FU resistance is just beginning to be appreciated. This review summarizes the current knowledge on the role of drug transporters with particular focus on ABC transporters in fluoropyrimidine-based chemotherapy response.
2012)TandutinibFLT3, PDGFR beta, and c-Kit++Yang et al. Vaidhyanathan et al. Minocha et al. (2012a)VemurafenibBRAF+++Durmus et al. , not determined. , 2011). Lagas, van Waterschoot, et al. (2009) found that Abcb1a/1b, but not Abcg2, limits oral uptake of dasatinib. 0-fold in the absence of both transporters. , 2014). This indicates that oral uptake of crizotinib was restricted only by Abcb1a/1b and that this Abcb1a/1b activity was saturable. In vitro, crizotinib was an ABCB1 but not an Abcg2 substrate.
ABC Transporters and Cancer by Toshihisa Ishikawa, John Schuetz