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The ruthenium drug and GRP78 inhibitor KP1339/IT-139 has already demonstrated promising anticancer activity in a phase I clinical trial. This study aimed to identify mechanisms underlying increased sensitivity to KP1339 treatment. Based on a screen utilizing 23 cell lines, a small panel was selected to compare KP1339-sensitive and low-responsive models. KP1339 sensitivity was neither based on differences...
The Ru(III) complex salt KP1019 induced formation of H 2 O 2 in colorectal tumor cells in a dose-dependent way. It also caused DNA-strand breaks if only weakly doubling tail length to 55.87±3.97μm. Both effects were prevented by 5mM N-acetylcysteine (NAC) which also reduced cytotoxicity (IC 50 55 vs 30μM without NAC). Induction of apoptosis was shown by loss of mitochondrial...
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