By Toshihisa Ishikawa, John Schuetz
ABC Transporters and Cancer offers necessary details at the interesting and fast-moving box of melanoma examine. the following, impressive and unique reports are offered on a number of issues. This quantity covers ABC transporters and melanoma, and is acceptable for researchers and scholars alike.
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Extra info for ABC Transporters and Cancer
The first mammalian drug resistance ABC transporter, P-glycoprotein (aka P-gp, MDR1, ABCB1), functionally identified almost 40 years ago, heralded the idea that most forms of impaired tumor response to chemotherapy (drug resistance) would be accounted for by this one protein. , nucleosides, antifolates, and camptothecins) were not exported by P-glycoprotein. As we moved forward, a more complex contemporary view of ABC transporters in cancer chemotherapy has evolved. The role of ABC transporters in cancer can now be viewed from multiple complementary perspectives, all of which are likely to impact therapeutic response.
This was a similar oral bioavailability as observed in Abcb1a/1b-knockout mice in the same experiment. These experiments thus show that elacridar is an effective in vivo Abcb1a/1b inhibitor and results in almost complete uptake of paclitaxel from the intestinal tract. Cyclosporin A and valspodar are more modest inhibitors, resulting in lower uptake rates (Bardelmeijer, Ouwehand, Beijnen, Schellens, & van Tellingen, 2004). , 2014). Elacridar boosting was studied not only in mice but also in rats.
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. But also tumor efficacy of orally administered taxanes has been evaluated when coadministered with Abcb1a/1b inhibitors. , 2002). But in the same experiment, it was also found that oral coadministration of paclitaxel (50 or 100 mg/kg) and dofequidar resulted in comparable antitumor efficacy as a single dose of intravenously administered paclitaxel (20 mg/kg).