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Updated: Mar 23, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Multi-kinase inhibitors, AURKs and cancer
Jonas Cicenas1,2,3,4, Erikas Cicenas5
1University of Bern, Vetsuisse Faculty, Institute of Animal Pathology, 3012, Bern, Switzerland. j.cicenas@mapkinases.eu.
Abstract:
Inhibitors that impact function of kinases are valuable both for the biological research as well as therapy of kinase-associated diseases, such as different cancers. There are quite a number of inhibitors, which are quite specific for certain kinases and several of them are either already approved for the cancer therapy or are in clinical studies of various phases. However, that does not mean that each single kinase inhibitor is suitable for targeted therapy. Some of them are not effective others might be toxic or fail some other criteria for the use in vivo. On the other hand, even in case of successful therapy, many responders eventually develop resistance to the inhibitors. The limitations of various single kinase inhibitors can be fought using compounds which target multiple kinases. This tactics can increase effectiveness of the inhibitors by the synergistic effect or help to diminish the likelihood of drug resistance. To date, several families of kinases are quite popular targets of the inhibition in cancers, such as tyrosine kinases, cycle-dependent kinases, mitogen-activated protein kinases, phosphoinositide 3-kinases as well as their pathway "players" and aurora kinases. Aurora kinases play an important role in the control of the mitosis and are often altered in diverse human cancers. Here, we will describe the most interesting multi-kinase inhibitors which inhibit aurora kinases among other targets and their use in preclinical and clinical cancer studies.
Insights
Multi-kinase inhibitors targeting aurora kinases offer enhanced cancer therapy by increasing effectiveness and reducing drug resistance. These compounds show promise in preclinical and clinical studies for treating various cancers.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Kinase inhibitors are crucial for cancer research and therapy, with many specific inhibitors approved or in clinical trials.
- Limitations of single kinase inhibitors include ineffectiveness, toxicity, and the development of drug resistance in patients.
- Targeting multiple kinases simultaneously offers a strategy to overcome these limitations through synergistic effects and reduced resistance.
Purpose of the Study:
- To review multi-kinase inhibitors that target aurora kinases alongside other kinases.
- To discuss the application of these inhibitors in preclinical and clinical cancer studies.
- To highlight the potential of multi-targeting strategies in cancer treatment.
Main Methods:
- Review of scientific literature on multi-kinase inhibitors.
- Analysis of preclinical and clinical study data for inhibitors targeting aurora kinases.
- Focus on compounds inhibiting aurora kinases and additional kinase targets.
Main Results:
- Several multi-kinase inhibitors targeting aurora kinases have demonstrated potential in cancer therapy.
- These inhibitors can enhance treatment efficacy and potentially overcome resistance mechanisms.
- Promising results observed in various preclinical and clinical investigations.
Conclusions:
- Multi-kinase inhibitors targeting aurora kinases represent a promising therapeutic strategy for diverse cancers.
- Simultaneous inhibition of multiple kinases can improve treatment outcomes and combat drug resistance.
- Further clinical development of these agents is warranted for effective cancer treatment.
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