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Updated: Jun 30, 2026
Assaying Protein Kinase Activity with Radiolabeled ATP
Published on: May 26, 2017
Recent advances in methods to assess the activity of the kinome
Maria Radu1, Jonathan Chernoff1
1Cancer Biology Program, Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA, 19111-2497, USA.
Abstract:
Protein and lipid kinases are deregulated in most, if not all, cancers and are among the most valuable therapeutic targets in these diseases. Despite the introduction of dozens of effective kinase inhibitors into clinical practice, the development of drug resistance remains a major barrier to treatment because of adaption of cellular signaling pathways to bypass targeted kinases. So that the basal and adaptive responses of kinases in cancer can be better understood, new methods have emerged that allow simultaneous and unbiased measurement of the activation state of a substantial fraction of the entire kinome. Here, we discuss such kinome-profiling methodologies, emphasizing the relative strengths and weaknesses of each approach.
Insights
Kinases are key cancer targets, but drug resistance is a problem. New kinome-profiling methods help understand kinase activity and resistance, aiding cancer therapy development.
Area of Science:
- Biochemistry
- Oncology
- Molecular Biology
Background:
- Protein and lipid kinases are frequently deregulated in cancers, representing critical therapeutic targets.
- Drug resistance due to adaptive cellular signaling pathways bypassing targeted kinases is a major challenge in cancer treatment.
Purpose of the Study:
- To review and compare emerging kinome-profiling methodologies.
- To enhance understanding of basal and adaptive kinase responses in cancer.
Main Methods:
- Discussion of various kinome-profiling techniques.
- Emphasis on simultaneous and unbiased measurement of kinase activation states.
- Comparative analysis of the strengths and weaknesses of different approaches.
Main Results:
- Kinome-profiling enables comprehensive assessment of kinase activity.
- These methods offer insights into mechanisms of drug resistance.
- Understanding kinase signaling is crucial for overcoming therapeutic barriers.
Conclusions:
- Kinome-profiling technologies are advancing the study of cancer kinases.
- These methodologies are vital for developing strategies to combat kinase-targeted drug resistance.
- Further research using these tools will improve cancer treatment outcomes.
