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Updated: Jul 14, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Aurora-kinase inhibitors as anticancer agents
Nicholas Keen1, Stephen Taylor
1Cancer and Infection Research Area, AstraZeneca Pharmaceuticals, Mereside, Alderley Park, Cheshire, SK10 4TG, UK. Nick.Keen@astrazeneca.com
Abstract:
Errors in mitosis can provide a source of the genomic instability that is typically associated with tumorigenesis. Many mitotic regulators are aberrantly expressed in tumour cells. These proteins could therefore make useful therapeutic targets. The kinases Aurora-A, -B and -C represent a family of such targets and several small-molecule inhibitors have been shown to block their function. Not only have these inhibitors advanced our understanding of mitosis, but, importantly, their in vivo antitumour activity has recently been reported. What have these studies taught us about the therapeutic potential of inhibiting this family of kinases?
Insights
Errors in cell division (mitosis) can lead to genomic instability and cancer. Inhibiting Aurora kinases, which are key regulators of mitosis, shows promise as a cancer therapy due to their demonstrated in vivo anti-tumor activity.
Area of Science:
- Molecular Biology
- Cell Biology
- Cancer Research
Background:
- Genomic instability, often stemming from mitotic errors, is a hallmark of cancer.
- Aberrant expression of mitotic regulators in tumor cells presents therapeutic opportunities.
- Aurora kinases (A, B, and C) are crucial regulators of mitosis and are implicated in tumorigenesis.
Purpose of the Study:
- To review the therapeutic potential of inhibiting Aurora kinases (A, B, and C) in cancer treatment.
- To explore the insights gained from small-molecule inhibitors targeting Aurora kinases.
- To assess the in vivo anti-tumor activity of these inhibitors.
Main Methods:
- Review of studies involving small-molecule inhibitors of Aurora kinases.
- Analysis of research on the role of Aurora kinases in mitosis and cancer.
- Evaluation of in vivo data on the anti-tumor effects of Aurora kinase inhibition.
Main Results:
- Small-molecule inhibitors effectively block Aurora kinase function.
- These inhibitors have advanced the understanding of mitotic processes.
- Significant in vivo anti-tumor activity of Aurora kinase inhibitors has been reported.
Conclusions:
- Aurora kinases represent promising therapeutic targets for cancer treatment.
- Inhibition of Aurora kinases demonstrates potential for effective anti-cancer therapies.
- Further research into Aurora kinase inhibitors is warranted for clinical application.
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