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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
Nature Reviews. Cancer
|December 2, 2004
Summary
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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