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Updated: Feb 27, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening
Published on: August 29, 2015
Approaches to identify kinase dependencies in cancer signalling networks
Maria Dermit1, Arran Dokal1, Pedro R Cutillas1
1Cell Signalling & Proteomics Group, Barts Cancer Institute (CRUK Centre), Queen Mary University of London, UK.
Abstract:
Cells integrate extracellular signals into appropriate responses through a complex network of biochemical reactions driven by the activity of protein and lipid kinases, among other proteins. In order to understand this complexity, new approaches, both experimental and computational, have recently been developed with the aim to identify regulatory kinases and infer their activation status in the context of their signalling network. Here, we review such approaches with particular focus on those based on phosphoproteomics. Integration of kinase activity measurements inferred from phosphoproteomics data with other 'omics' datasets is starting to be used to identify regulatory nodes in biochemical networks. These methodologies may in the future be used to identify patient-specific targets and thus advance personalised cancer medicine.
Insights
New phosphoproteomics methods help identify regulatory kinases and their activation status in cell signaling networks. This approach advances personalized cancer medicine by pinpointing patient-specific targets.
Area of Science:
- Biochemistry
- Cell Biology
- Systems Biology
Background:
- Cells process external signals via complex biochemical networks.
- Kinases (protein and lipid) are key regulators in these signaling pathways.
- Understanding kinase activity is crucial for deciphering cellular responses.
Purpose of the Study:
- To review experimental and computational approaches for identifying regulatory kinases.
- To focus on phosphoproteomics-based methods for inferring kinase activation.
- To highlight the integration of phosphoproteomics with other omics data.
Main Methods:
- Review of phosphoproteomics-based methodologies.
- Integration of kinase activity data with other omics datasets (e.g., genomics, transcriptomics).
- Computational approaches for network analysis and regulatory node identification.
Main Results:
- Phosphoproteomics enables inference of kinase activation status within signaling networks.
- Integrating phosphoproteomics with other omics data aids in identifying key regulatory nodes.
- Emerging methodologies show promise for network-level kinase activity assessment.
Conclusions:
- Phosphoproteomics is a powerful tool for understanding kinase-driven signaling.
- Integrated omics approaches enhance the identification of regulatory elements in cellular networks.
- These advancements pave the way for personalized cancer medicine through target identification.
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