ABC Transporters and Cancer by Toshihisa Ishikawa, John Schuetz PDF

By Toshihisa Ishikawa, John Schuetz

ISBN-10: 0128013613

ISBN-13: 9780128013618

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.

  • Provides info on melanoma research
  • Outstanding and unique reviews
  • Suitable for researchers and students
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    Sample text

    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.

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    ABC Transporters and Cancer by Toshihisa Ishikawa, John Schuetz


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