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Updated: Jul 5, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Target validation and biomarker identification in oncology : the example of aurora kinases
Riccardo Colombo1, Jürgen Moll
1Nerviano Medical Sciences Srl, Nerviano, Italy.
Abstract:
The strong link between gene expression of mitotic Aurora kinases and cancer has stimulated a very high interest in developing Aurora kinase inhibitors for cancer therapy. Validation of Aurora kinases as targets, and development of pharmacodynamic biomarkers for inhibitors of Aurora kinases, provides an example of how target validation can help the drug discovery process, and also of how to interpret results depending on the technology used. In this review, we outline the principal tools, concepts, and strategies of target and biomarker validation for Aurora kinases, with emphasis on validation results derived from RNA-interference experiments. These data were essential for the decision to enter the next steps in drug development and for the selection of the appropriate biomarkers for clinical trials.
Insights
Targeting Aurora kinases is crucial for cancer therapy. This review details validating these kinases and their biomarkers, using RNA-interference data to guide drug development and clinical trials.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- The association between Aurora kinase gene expression and cancer drives interest in developing inhibitors.
- Aurora kinases are key regulators of mitosis, making them attractive cancer targets.
Purpose of the Study:
- To review strategies for validating Aurora kinases as drug targets.
- To discuss the development and interpretation of pharmacodynamic biomarkers for Aurora kinase inhibitors.
- To highlight the role of RNA-interference data in advancing drug discovery.
Main Methods:
- Review of target and biomarker validation tools and concepts.
- Emphasis on validation results from RNA-interference (RNAi) experiments.
- Analysis of data interpretation based on different technologies.
Main Results:
- RNA-interference data proved essential for progression to later drug development stages.
- Validation strategies informed the selection of biomarkers for clinical trials.
- Demonstrated how target validation aids the drug discovery process.
Conclusions:
- Effective validation of Aurora kinases and their biomarkers is critical for successful cancer drug development.
- RNA-interference studies provide valuable insights for therapeutic strategies.
- Biomarker selection based on robust validation is key for clinical trial success.
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