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Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein
Published on: June 30, 2019
Functional interrogation of the kinome using nucleotide acyl phosphates
Matthew P Patricelli1, A Katrin Szardenings, Marek Liyanage
1ActivX Biosciences, 11025 North Torrey Pines Road, La Jolla, California 92037, USA..
Biochemistry
|January 11, 2007
Summary
This study introduces a novel method using acyl phosphate probes to identify and quantify protein kinases in any biological sample. This approach aids in drug discovery by profiling kinase activity and assessing inhibitor selectivity.
Area of Science:
- Biochemistry
- Molecular Biology
- Proteomics
Background:
- Protein kinases are crucial in cell signaling and are key targets for various therapeutic applications.
- Existing methods for kinase identification and quantification have limitations in scope and applicability.
Purpose of the Study:
- To develop a universal method for identifying and quantifying protein kinases across diverse biological samples and species.
- To enable broad profiling of kinase activity for target discovery and inhibitor assessment.
Main Methods:
- Utilized acyl phosphate-containing nucleotides (biotin derivative with ATP or ADP) as probes.
- Probes selectively bind to the ATP-binding sites of protein kinases.
- Mass spectrometry-based analysis of captured, biotinylated peptide fragments to identify kinases and their levels.
Main Results:
- The method successfully identified and quantified protein kinases in various samples, reacting with at least 75% of known human protein kinases.
- Enabled direct assessment of inhibitor potency and selectivity against native protein kinases and other ATPases.
- Demonstrated broad profiling of kinase activities in native proteomes.
Conclusions:
- This novel acyl phosphate probe method offers a powerful tool for comprehensive kinase profiling.
- Facilitates both the discovery of new therapeutic targets and the evaluation of drug candidate selectivity.
- Represents a significant advancement in understanding kinase function in biological systems.
