By Toshihisa Ishikawa, John Schuetz
ABC Transporters and Cancer presents useful details at the intriguing and fast-moving box of melanoma learn. the following, awesome and unique reports are offered on quite a few subject matters. This quantity covers ABC transporters and melanoma, and is appropriate for researchers and scholars alike.
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These findings provide a better understanding of the importance of apical ABC transporters in chemotherapy and may therefore advance translation of promising preclinical insights and approaches to clinical studies. Keywords ABC transporters Chemotherapeutics Drug disposition Oral availability Brain disposition Abbreviations ABC ATP-binding cassette AUC area under the curve BBB blood–brain barrier CNS central nervous system EGFR epidermal growth factor receptor FGFR fibroblast growth factor receptor JAK Janus kinase MDR multidrug resistance mTOR mammalian target of rapamycin PDGFR platelet-derived growth factor receptor RET rearranged during transfection TKI tyrosine kinase inhibitor VEGFR vascular endothelial growth factor receptor WT wild type 1 Introduction to Apical ABC Transporters ATP-binding cassette (ABC) transporters are active multispanning transmembrane protein pumps that, in higher organisms, are widely expressed in a broad range of membranes of tissues.
Herbal extracts containing compounds such as curcumin, resveratrol, and silibinin are often used as complementary and alternative medicines (CAMs) in cancer (Klempner & Bubley, 2012; Philippou, Hadjipavlou, Khan, & Rane, 2013). , 2010; Li & Paxton, 2013). These extracts and their active substances are therefore often combined with orally administered taxanes in preclinical studies to inhibit (intestinal) Abcb1a/1b and to boost oral availability of taxanes. 4%) (Choi, Choi, & Shin, 2004). , 2012), silymarin (Park, Park, Hur, Woo, & Lee, 2012), and its main component silibinin (Lee & Choi, 2010).
2012)Trametinib+++–Vaidhyanathan et al. (2014)Vandetanib++++ElacridarFivefoldbMinocha et al. (2012a)Veliparib++++ElacridarCompleteaLin et al. (2014)Vemurafenib+++++ElacridarPartial (~ 59%)aDurmus et al. (2012) If available, effect of using pharmacological inhibitors of the ABC transporters on brain penetration is also presented. a Relative to vehicle-treated Abcb1a/1b;Abcg2−/− mice. b Data available only in WT mice where brain-to-plasma ratios were compared between elacridar- and vehicle-treated groups.