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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
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Light-assisted small-molecule screening against protein kinases.
Álvaro Inglés-Prieto1, Eva Reichhart1, Markus K Muellner2
1Institute of Science and Technology Austria (IST Austria), Klosterneuburg, Austria.
Nature Chemical Biology
|October 13, 2015
Summary
We developed an all-optical screening method using optogenetics for faster, more informative drug discovery. This approach eliminates chemical activators and reporters, streamlining cell-based assays for protein kinases.
Area of Science:
- Systems biology
- Drug discovery
- Optogenetics
Background:
- High-throughput live-cell screens are crucial for systems biology and drug discovery.
- Current methods often rely on chemical activators and reporters, adding complexity.
- There is a need for streamlined, information-rich screening platforms.
Purpose of the Study:
- To demonstrate an optogenetics-assisted method for cell-based screening.
- To reduce operational steps and increase information content in screening assays.
- To provide a blueprint for all-optical screening adaptable to various drug targets.
Main Methods:
- Developed an optogenetics-based screening approach.
- Applied the method to a cell-based small-molecule screen against human protein kinases.
- Included screening against an orphan receptor tyrosine kinase.
Main Results:
- The optogenetics-assisted method avoids chemical activators and reporters.
- The new method reduces the number of operational steps.
- Increased information content was observed in the cell-based screen.
Conclusions:
- An all-optical screening blueprint using optogenetics is presented.
- This method offers an efficient alternative to traditional chemical screening.
- The approach is adaptable to diverse drug targets and cellular processes.
