Protein kinases screening

Enzyme-adduct formation has also been successfully achieved with the Erbl and 2 (receptor tyrosine kinases from EGFR subfamily) [19, 20], suggesting that the tethered library-screening approach would also be amenable to protein kinases. 

Fig. 1.6 The increase in potency of a 1.3 mM p38 a protein kinase-binding fragment inhibitor identified by X-ray screening through the major changes made to the chemical series to exploit key binding features within the active site.

The abundance of crystallographic information on the 3D structure of protein kinases, including knowledge of receptor-ligand complexes, has seen protein kinases feature consistently in datasets employed to both develop and evaluate methods for receptor-based screening. Indeed, the vast majority of literature surrounding protein kinases and receptor-based in silico... 

Kashem, M., Yingling, J., Nelson, R., and Homon, C., New tools for screening protein kinases a comparative study, presented at 9th Annual Conference and Exhibition of the Society for Biomolecular Screening, Portland, OR, September 21-25, 2003. 

In 2006, Greis and co-workers reported on the application of MALDI-TOF MS as a tool for rapid inhibitor screening [10]. Different kinases (protein kinase C-a, cAMP-dependent protein kinase) in combination with their substrates were assayed, and the inhibitory potencies of staurosporine and three novel compounds were determined. For all four compounds, IC50 values could be determined, and... 

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