Related Experiment Video
Updated: Mar 27, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Aurora Kinase Inhibitors: Current Status and Outlook
Vassilios Bavetsias1, Spiros Linardopoulos2
1Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , London , UK.
Abstract:
The Aurora kinase family comprises of cell cycle-regulated serine/threonine kinases important for mitosis. Their activity and protein expression are cell cycle regulated, peaking during mitosis to orchestrate important mitotic processes including centrosome maturation, chromosome alignment, chromosome segregation, and cytokinesis. In humans, the Aurora kinase family consists of three members; Aurora-A, Aurora-B, and Aurora-C, which each share a conserved C-terminal catalytic domain but differ in their sub-cellular localization, substrate specificity, and function during mitosis. In addition, Aurora-A and Aurora-B have been found to be overexpressed in a wide variety of human tumors. These observations led to a number of programs among academic and pharmaceutical organizations to discovering small molecule Aurora kinase inhibitors as anti-cancer drugs. This review will summarize the known Aurora kinase inhibitors currently in the clinic, and discuss the current and future directions.
Insights
Aurora kinases are crucial for cell division, and their dysregulation is linked to cancer. This review covers small molecule inhibitors targeting these kinases for cancer therapy.
Area of Science:
- Molecular Biology
- Cell Biology
- Biochemistry
Background:
- Aurora kinases (A, B, and C) are serine/threonine kinases critical for mitosis.
- Their activity and expression peak during cell division, regulating key mitotic events.
- Overexpression of Aurora-A and Aurora-B is common in human tumors.
Purpose of the Study:
- To review small molecule inhibitors of Aurora kinases.
- To discuss inhibitors currently in clinical trials for cancer treatment.
- To explore future directions in Aurora kinase inhibitor development.
Main Methods:
- Literature review of published studies on Aurora kinase inhibitors.
- Analysis of clinical trial data for Aurora kinase inhibitors.
- Synthesis of information on inhibitor mechanisms and therapeutic potential.
Main Results:
- Several small molecule inhibitors targeting Aurora kinases have been developed.
- These inhibitors are progressing through various phases of clinical trials.
- Challenges and opportunities in Aurora kinase inhibitor therapy are identified.
Conclusions:
- Aurora kinase inhibitors represent a promising therapeutic strategy for various cancers.
- Further research is needed to optimize inhibitor efficacy and minimize side effects.
- Targeting Aurora kinases holds potential for future cancer treatment advancements.
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