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Updated: Mar 1, 2026
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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
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Biosensors for Screening Kinase Inhibitors
Nikhil Bhalla1, Pedro Estrela2
1Okinawa Institute of Science and Technology Graduate University (OIST) 1919-1 Tancha, Onna, Kunigami District, Okinawa Prefecture 904-0412, Japan.
Current Topics in Medicinal Chemistry
|June 1, 2017
Summary
Protein phosphorylation, regulated by kinases, is key in diseases like Alzheimer's, diabetes, and cancer. This review covers technologies for detecting kinase activity and finding new kinase inhibitors for drug discovery.
Area of Science:
- Biochemistry and Molecular Biology
- Pharmacology and Drug Discovery
Background:
- Protein phosphorylation is a critical post-translational modification in eukaryotic cells.
- Dysregulation of protein phosphorylation is implicated in major diseases, including Alzheimer's disease, diabetes, and various cancers.
- Kinases facilitate protein phosphorylation, making them key targets for therapeutic intervention.
Purpose of the Study:
- To review technologies for detecting kinase activity.
- To discuss methods for screening compounds to identify novel protein kinase inhibitors.
- To highlight the role of kinase inhibitors in managing diseases linked to aberrant phosphorylation.
Main Methods:
- Review of current literature on kinase activity detection technologies.
- Analysis of high-throughput screening (HTS) methodologies for kinase inhibitor discovery.
- Discussion of established and emerging techniques for compound screening.
Main Results:
- Identification of diverse technologies for monitoring kinase enzymatic activity.
- Overview of strategies for identifying small molecules that inhibit kinase function.
- Emphasis on the importance of robust screening platforms in drug development.
Conclusions:
- Understanding kinase function and developing specific inhibitors are crucial for treating diseases driven by protein phosphorylation.
- Technological advancements in kinase activity detection and compound screening accelerate the drug discovery pipeline.
- Targeting kinases offers a promising therapeutic avenue for Alzheimer's disease, diabetes, and cancer.
