Searchable database of kinase specificity data for ~200 widely used kinase inhibitors now available on MRC-PPU website


http://www.kinase-screen.mrc.ac.uk/kinase-inhibitors



Protein kinases are one of the pharmaceutical industry's most important classes of drug target. Nineteen protein kinase inhibitors have been approved for clinical use and over 150 more are undergoing clinical trials of which about 25 are in Phase III. A major challenge in this area is to develop a drug that selectively suppresses the activity of one, or at most a few, of the 500 protein kinases encoded by the human genome.



The MRC Protein Phosphorylation Unit (MRC-PPU) at Dundee pioneered analysis of the selectivity of protein kinase inhibitors by setting up the first service to tackle this problem in 1998. This procedure, termed 'kinase profiling' proved to be of great help to the pharmaceutical industry, speeding up the development of specific protein kinase inhibitors with therapeutic potential.



In order to enable academic drug discovery efforts and pharmaceutical companies to access kinase profiling services at an affordable price the MRC-PPU has set up the International Centre for Kinase Profiling to analyse the specificity of protein kinase inhibitors against a panel of nearly 150 protein kinases.

To help the research community select the optimal kinase inhibitors for biological studies and to make researchers aware of the limitations of many widely used kinase inhibitors we have generated a new searchable database of the inhibitor specificities of over 200 of the most commonly used signal transduction inhibitors.



We strongly recommend undertaking kinase profiling of any kinase inhibitor to be used in a biological experiment. It is essential to have a good feel for the specificity of the kinase inhibitor you are working with in order to be able to properly interpret your data.



If you have additional kinase inhibitors you are working with that have not been subject to kinase profiling and would like the International Centre for Kinase Profiling team to profile these for you please contact us at kinase-screen@dundee.ac.uk and see our website for further details.

Note that the International Centre for Kinase Profiling team also offers lipid kinase profiling against 16 lipid kinases.