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| SynKinase Newsletter Jan 2012 |
| A kinase interaction map profiling the activity of 178 commercially available kinase inhibitors against a panel of 300 recombinant kinases from over 100,00 independent functional assays was recently reported in Nature Biotechnology 29, 1039-1045, 2011 (doi: 10.1038/nbt.2017) by Jeffrey R. Peterson, Ph.D., and colleagues at the Fox Chase Cancer Center. *************************************************************************** ********************************************************************************************
Protein kinases represent important therapeutic targets because of their key roles in cell signaling, but designing selective inhibitors has been a challenge. Owing to evolutionary conservation of the ATP-binding site, which represents a useful target epitope for most kinase inhibitors, individual inhibitors are likely to promiscuously inhibit multiple kinases. This report revealed complex and often unexpected interactions between protein kinases and kinase inhibitors, with a wide spectrum of promiscuity. Many off-target interactions occur with seemingly unrelated kinases, revealing how large-scale profiling can identify multitargeted inhibitors of specific, diverse kinases. This finding has a remarkable impact on drug discovery and development in kinase area, as current selectivity assessment of newly identified kinase inhibitors is often carried out by testing against a limited panel of closely related kinases, based on the assumption that any off-target inter¬actions that occur will most likely impact on kinases with similar amino acid sequence. The results from this report provide a resource for selecting compounds to elucidate kinase function and for interpreting the results of experiments involving kinase inhibitors. (http://www.nature.com/nbt/journal/v29/n11/abs/nbt.2017.html)************************ *********************************************************************************************
Synkinase supplies a kinase array which consists of 96 kinase inhibitors at 0.5mg or 1mg in standard 96-well plate. Synkinase is currently offering heavy discount (30%) if client orders 0.5mg or 1mg sample of all 141 kinase inhibitors in our stock. This offer expires on 31Mar2012. |
| Date:2012-01-17 |
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| New! SUBSCRIPTION SERVICE |
| Agree to a minimum monthly purchase value and receive substantial discounts on all kinase inhibitors. For details, email us at: orders @ synkinase.com with 'subscription service' in the subject line. |
| Date:2010-09-14 |
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SynKinase Newsletter Jan 2012
A kinase interaction map profiling the activity of 178 commercially available kinase inhibitors agai... |
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