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Updated: Jun 24, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Aurora kinase inhibitors in preclinical and clinical testing
Chun Hei Antonio Cheung1, Mohane Selvaraj Coumar, Hsing-Pang Hsieh
1Institute of Cancer Research, National Health Research Institutes, Tainan, Taiwan, ROC.
Background:
Mitosis is a key step in the cell cycle governing the distribution of genetic material to the daughter cells. Any aberration in this process could lead to genomic instability. Aurora A, B and C, are members of the serine/threonine kinase family. Aurora kinases are essential for spindle assembly, centrosome maturation, chromosomal segregation and cytokinesis during mitosis. Abnormalities in the mitotic process through overexpression/amplification of aurora kinase have been linked to genomic instability leading to tumorigenesis. Hence, use of aurora kinase small molecule inhibitors as potential molecular-targeted therapeutic intervention for cancer is being pursued by various researchers.
Objective:
To review the literature of aurora kinase inhibitors in clinical and preclinical testing.
Method:
Pubmed, Scifinder and (www.clinicaltrials.gov) databases were used to search the literature for aurora kinase. CONCLUSION/RESULTS: Approximately 13 aurora kinase inhibitors are under Phase I/II evaluation at present for various cancers of different origins; and several others are in preclinical testing. Details of their preclinical/clinical results and important considerations for future aurora kinase inhibitor development are discussed. Considering the fact that aurora kinase plays an important role in the mitosis process and is involved in tumorigenesis, development of aurora kinase inhibitors for the treatment of cancer, either as a single agent or in combination with existing cancer treatment is warranted.
Insights
Aurora kinase inhibitors are crucial for targeting mitotic errors and genomic instability in cancer. This review highlights 13 inhibitors in clinical trials, supporting their development for cancer therapy.
Area of Science:
- Cell Biology
- Molecular Oncology
- Drug Discovery
Background:
- Mitosis is essential for cell division; errors can cause genomic instability.
- Aurora kinases (A, B, C) are critical for mitosis, and their dysregulation is linked to cancer.
- Targeting aurora kinases offers a potential molecular-based cancer therapy.
Purpose of the Study:
- To review existing literature on aurora kinase inhibitors.
- To assess their clinical and preclinical development status.
Main Methods:
- Literature search conducted using PubMed, SciFinder, and clinicaltrials.gov.
- Focused on aurora kinase inhibitors in cancer research.
Main Results:
- Approximately 13 aurora kinase inhibitors are in Phase I/II clinical trials.
- Numerous other inhibitors are undergoing preclinical testing.
- Preclinical and clinical data are being evaluated for future development.
Conclusions:
- Aurora kinase inhibitors show promise for cancer treatment.
- Further development is warranted, potentially in combination therapies.
- Targeting aurora kinase is a key strategy for combating tumorigenesis.
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