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A Flexible Workflow for Automated Bioluminescent Kinase Selectivity Profiling
Tracy Worzella1, Matt Butzler1, Jacquelyn Hennek1,2
11 Promega Corporation, R&D Department, Madison, WI, USA.
SLAS Technology
|January 18, 2017
Summary
This study presents an automated kinase profiling workflow for drug discovery, enabling researchers to efficiently assess inhibitor selectivity and off-target activities in-house. The streamlined process confirms known interactions and identifies novel ones, accelerating compound evaluation.
Area of Science:
- Biochemistry
- Drug Discovery
- Assay Development
Background:
- Kinase profiling is crucial for drug discovery to ensure inhibitor selectivity and identify off-target effects.
- In-house kinase profiling is often limited by cost and logistical challenges.
Purpose of the Study:
- To develop an automated, flexible, and cost-effective kinase profiling workflow for in-house use.
- To streamline the process of assessing compound-kinase interactions and off-target activities.
Main Methods:
- Utilized ready-to-use kinase enzymes and substrates in convenient eight-tube strips.
- Employed a bench-top liquid handling device (Gilson PIPETMAX) for automated reaction assembly.
- Integrated ADP-Glo Kinase Assay technology and a multimode detection instrument (GloMax Discover) for luminescence detection and data analysis.
Main Results:
- Developed customized pipetting protocols adaptable to user-defined parameters (compound number, titration increments, kinase families).
- Successfully confirmed known target-specific inhibitions.
- Identified and validated novel small molecule-kinase interactions, including previously unknown off-target inhibitions.
Conclusions:
- The automated workflow enables rapid and efficient on-site kinase profiling.
- This streamlined process facilitates quicker compound evaluation and decision-making in drug discovery programs.
