2015
DOI: 10.1093/annonc/mdv293
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Inhibition of the spindle assembly checkpoint kinase TTK enhances the efficacy of docetaxel in a triple-negative breast cancer model

Abstract: The compound is characterized by long residence time on the target and inhibits the proliferation of a wide variety of human cancer cell lines with potency in the same range as marketed cytotoxic agents. In cell lines and in mice, NTRC 0066-0 inhibits the phosphorylation of a TTK substrate and induces chromosome missegregation. NTRC 0066-0 inhibits tumor growth in MDA-MB-231 xenografts as a single agent after oral application. To address the effect of the inhibitor in breast cancer, we used a well-defined mous… Show more

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Cited by 108 publications
(158 citation statements)
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“…In addition, the combination of IN-3 and vincristine led to almost complete tumor shrinkage and prolonged survival in orthotopic GBM mouse models 15 . Therefore, we concluded that selective MPS1 inhibition sensitizes GBM cells to the effects of antimitotic drugs, an assumption supported by data reported by other groups 2528 .…”
Section: Discussionsupporting
confidence: 86%
“…In addition, the combination of IN-3 and vincristine led to almost complete tumor shrinkage and prolonged survival in orthotopic GBM mouse models 15 . Therefore, we concluded that selective MPS1 inhibition sensitizes GBM cells to the effects of antimitotic drugs, an assumption supported by data reported by other groups 2528 .…”
Section: Discussionsupporting
confidence: 86%
“…Extremely shortened mitosis induces massive chromosome missegregation and/or tetraploidization that elevates cell stress beyond the lethal level [164,165]. In line with the idea, inhibitors of Mps1 kinase were shown to exert anti-tumor activities [166][167][168], and anti-SAC compounds were reported to sensitize cancer cells to microtubule-targeting drugs [169][170][171][172].…”
Section: Accepted Manuscriptmentioning
confidence: 98%
“…NTRC 0066-0 0.6 nM (Maia et al, 2015) Chromosome missegregation Breast cancer (Maia et al, 2015) Short mitotic duration (Maia et al, 2015) Reversine 3 nM Chromosome misalignment Dou et al, 2015) Failure in recruitment of Mad1, Bub1, BubR1 and Rod-Zw10-Zwilch Defect in MCC assembly (Tipton et al, 2013) Short mitotic duration Hyperploidy (Jemaa et al, 2012a) Apoptosis (Jemaa et al, 2012a;Jemaa et al, 2016) SP600125 692 nM (Schmidt et al, 2005) Failure in BubR1 recruitment (Schmidt et al, 2005) SAC bypass (Schmidt et al, 2005) Apoptosis ( …”
Section: Chromosome Misalignment and Missegregationmentioning
confidence: 99%