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Protein kinases constitute a family of more than 500 proteins in humans with central functions in most aspects of life. Due to their key roles in cellular signalling, dysregulation of kinases is frequently associated with disease and inhibitors have been developed for a considerable number of them. Although kinases are well established drug targets many of the developed kinase inhibitors lack selectivity over related kinases making them less useful tools for biological experiments to explore the activity of a specific kinase. In addition there is a large number of kinases ‘the untargeted kinome’ for which no potent, specific and cell active inhibitors ‘probes’ are available.
Goals
- to develop chemical probes for protein kinases
- to share chemical probes with the research community
- to create a comprehensive chemogenomics set
Susanne Muller-Knapp coordinates the Kinase Chemical Probe Program.
| SGC Site | Lead Investigator | Primary Capabilities | Primary Focus |
| Campinas | Rafael Couñago | Protein expression X-ray crystallography Medicinal chemistry Cell assays
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RNA splicing In-house kinase profiling
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UNC |
Tim Willson | Medicinal chemistry Compound sets |
Chemical probes Chemogenomics |
| Oxford | Alex Bullock Jon Elkins |
Protein expression X-ray crystallography Screening Cell assays |
Chemical biology |
| Frankfurt | Stefan Knapp | Screening X-ray crystallography Medicinal chemistry Cell assays |
Chemical biology Chemical probes |
