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Updated: Jun 27, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Aurora-B kinase inhibitors for cancer chemotherapy
Sai-Ching Jim Yeung1, Christopher Gully, Mong-Hong Lee
1UT M. D. Anderson Cancer Center, 1515 Holcombe Blvd., Unit 079, Houston, Texas 77030, USA.
Abstract:
Cancer cells undergo mitosis frequently, and many mitotic regulators are aberrantly expressed in these cells. Members of the Aurora family of serine/threonine kinases are expressed during mitosis and carry out vital functions in chromosome alignment, segregation and cytokinesis. Here we review the functions of Aurora-B kinases in mitosis and summarize the current literature on Aurora-B kinase inhibitors. In the process of developing these inhibitors as anticancer drugs, the Aurora kinase inhibitors have also helped to advance our understanding of the role of Aurora kinases in mitosis. The mechanism of action and structure-activity relationship of a selective Aurora-B inhibitor are also discussed. The future may see mechanism guided design of chemotherapy combinations that include these cell-cycle phase-specific drugs. The therapeutic potential of Aurora-B inhibitors is promising.
Insights
Aurora-B kinase inhibitors are promising anticancer drugs that target cell division. Research on these inhibitors enhances understanding of Aurora kinases in mitosis and guides future chemotherapy combinations.
Area of Science:
- Molecular Biology
- Cell Biology
- Oncology
Background:
- Cancer cells exhibit frequent mitosis with aberrant expression of mitotic regulators.
- Aurora kinases, including Aurora-B, are crucial serine/threonine kinases regulating mitosis.
- Dysregulation of Aurora kinases is implicated in cancer development.
Purpose of the Study:
- To review the functions of Aurora-B kinases in mitosis.
- To summarize the current literature on Aurora-B kinase inhibitors.
- To discuss the mechanism of action and structure-activity relationship of selective Aurora-B inhibitors.
Main Methods:
- Literature review of studies on Aurora-B kinase functions and inhibitors.
- Analysis of existing data on Aurora kinase inhibitors in cancer therapy.
- Discussion of structure-activity relationships for selective Aurora-B inhibitors.
Main Results:
- Aurora-B kinases play vital roles in chromosome alignment, segregation, and cytokinesis.
- Aurora kinase inhibitors are being developed as anticancer drugs.
- Inhibitor development has advanced the understanding of Aurora kinase functions in mitosis.
Conclusions:
- Aurora-B kinase inhibitors show promising therapeutic potential in cancer treatment.
- Mechanism-guided design of chemotherapy combinations including these drugs is a future direction.
- These cell-cycle phase-specific drugs offer a targeted approach to cancer therapy.
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