1.BPR1K653, a novel Aurora kinase inhibitor, exhibits potent anti-proliferative activity in MDR1 (P-gp170)-mediated multidrug-resistant cancer cells.
Cheung CH1, Lin WH, Hsu JT, Hour TC, Yeh TK, Ko S, Lien TW, Coumar MS, Liu JF, Lai WY, Shiao HY, Lee TR, Hsieh HP, Chang JY. PLoS One. 2011;6(8):e23485. doi: 10.1371/journal.pone.0023485. Epub 2011 Aug 24.
BACKGROUND: Over-expression of Aurora kinases promotes the tumorigenesis of cells. The aim of this study was to determine the preclinical profile of a novel pan-Aurora kinase inhibitor, BPR1K653, as a candidate for anti-cancer therapy. Since expression of the drug efflux pump, MDR1, reduces the effectiveness of various chemotherapeutic compounds in human cancers, this study also aimed to determine whether the potency of BPR1K653 could be affected by the expression of MDR1 in cancer cells.