2007
DOI: 10.1517/14728222.12.1.69
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Abstract: Aurora kinases are key regulators of mitosis and inhibitors being developed by a wide range of pharmaceutical and biotechnology companies for the treatment of cancer. Tumor cells respond differentially on inhibition of different Aurora kinase family members and these differences have to be considered in the clinical development of small-molecule inhibitors with respect to the chosen indications, the schedules or the selection of appropriate end points and they should also guide the development of biomarkers. P… Show more

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Cited by 49 publications
(21 citation statements)
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References 86 publications
(86 reference statements)
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“…In some of the phase I trials described in this review, phosphorylation of histone H3 was used as a biomarker [73,84,121,122]. This event is associated with aurora B activity, since aurora B directly phosphorylates histone H3 on serine 10, making it a useful tool for evaluating the degree of aurora B inhibition [123,124]. Histone H3 phosphorylation is critical for the transformation of cancer cells, and might therefore be an anticancer target on its own [125].…”
Section: Discussionmentioning
confidence: 99%
“…In some of the phase I trials described in this review, phosphorylation of histone H3 was used as a biomarker [73,84,121,122]. This event is associated with aurora B activity, since aurora B directly phosphorylates histone H3 on serine 10, making it a useful tool for evaluating the degree of aurora B inhibition [123,124]. Histone H3 phosphorylation is critical for the transformation of cancer cells, and might therefore be an anticancer target on its own [125].…”
Section: Discussionmentioning
confidence: 99%
“…As our patient cohort included only metastatic patients, we hypothesize that AURKA may impact early stages of colorectal cancer, whereas AURKB has a role in metastatic disease. In fact, Katayama et al 32 reported AURKB expression levels to be closely related with Dukes' stage, as expression seemed to be increased in samples with a higher grade of malignancy.…”
Section: Discussionmentioning
confidence: 99%
“…1 Selective inhibition of Aurora A results in inhibition of autophosphorylation of Aurora A at Thr288, inhibition of p53 phosphorylation, monopolar spindles and G2-M arrest. 2,3 Human Aurora B kinase forms a chromosomal passenger complex (CPC) with three non-enzymatic subunits: inner centromere protein, survivin and borealin. 4 The highly dynamic CPC is critical for chromosome condensation, chromosome orientation on the mitotic spindle and the spindle-assembly checkpoint as well as the final stages of cytokinesis.…”
Section: Introductionmentioning
confidence: 99%
“…1 Selective inhibition of Aurora B classically results in polyploidy (X4 N DNA content due to DNA replication without cell division), inhibition of histone H3 phosphorylation at serine 10 and apoptosis. 2,3 Inhibition of phosphorylated histone H3 has also proved useful in the clinic as a mechanism of action biomarker for inhibition of Aurora B. 3 The gene for Aurora B, AURKB, maps to chromosome region 17p13.1.…”
Section: Introductionmentioning
confidence: 99%
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