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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
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Protein kinase profiling assays: a technology review.
1Reaction Biology Corp., One Great Valley Parkway, Suite 2, Malvern, PA 19355, USA.
Drug Discovery Today. Technologies
|January 3, 2016
Summary
Protein kinase profiling is crucial for drug discovery, aiding target selection and toxicity prediction. High-throughput screening assays are standard for evaluating compounds against kinase panels.
Area of Science:
- Biochemistry
- Pharmacology
- Drug Discovery
Background:
- Protein kinases are key drug targets for cancer and inflammatory diseases.
- Kinase profiling assesses compound selectivity across the kinome.
- Understanding selectivity aids target selection, compound prioritization, and toxicity assessment.
Purpose of the Study:
- To highlight the importance of kinase profiling in modern drug discovery.
- To discuss the role of comprehensive kinase screening in identifying potential therapeutics.
Main Methods:
- Utilizing kinase profiling to understand compound selectivity trends.
- Employing high-throughput screening (HTS) technologies against kinase panels.
- Screening compounds against diverse kinase panels and their mutants.
Main Results:
- Kinase profiling provides insights into general selectivity trends of lead compounds.
- Comprehensive screening is a standard approach in current drug discovery.
- Numerous HTS-compatible assays and technologies have been developed for kinase screening.
Conclusions:
- Kinase profiling is essential for informed drug target selection and compound evaluation.
- The development of HTS assays facilitates efficient screening against kinases.
- Standardized screening approaches are vital for advancing drug discovery pipelines.

