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Access through your institution Buy or subscribe Most small-molecule kinase inhibitors interact with multiple members of the protein kinase family; achieving selective inhibition of specific
protein kinases is challenging. These two papers describe studies of kinase inhibitor selectivity. Anastassiadis _et al_. profiled the activity of 178 kinase inhibitors against a panel of
300 protein kinases. They identified kinases that were inhibited by many compounds, as well as kinases that were resistant to small-molecule inhibition, and showed that many off-target
interactions occur with seemingly unrelated kinases. They also identified potential lead compounds for orphan kinases and for the development of multitargeted kinase inhibitors. Davis _et
al_. tested the interaction of 72 kinase inhibitors with 442 kinases. They showed that, as a group, type II inhibitors — which bind adjacently to the ATP site and prefer an inactive kinase
conformation — were generally more selective than type I inhibitors but several individual type I inhibitors were among the most selective identified. Furthermore, they identified a class of
inhibitors that was broadly active against a single subfamily of kinases but selective outside that subfamily, and several compounds that were active against orphan kinases. Together, these
papers provide information that could aid the identification of selective kinase inhibitors for use as tool compounds, and assist in kinase inhibitor drug discovery. This is a preview of
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ADDITIONAL ACCESS OPTIONS: * Log in * Learn about institutional subscriptions * Read our FAQs * Contact customer support ORIGINAL RESEARCH PAPERS * Anastassiadis, T. et al. Comprehensive
assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. _Nature Biotech._ 29, 1039–1045 (2011) Article CAS Google Scholar * Davis, M. I. et al. Comprehensive
analysis of kinase inhibitor selectivity. _Nature Biotech._ 29, 1046–1051 (2011 Article CAS Google Scholar Download references Authors * Charlotte Harrison View author publications You
can also search for this author inPubMed Google Scholar RIGHTS AND PERMISSIONS Reprints and permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Harrison, C. Analysing kinase inhibitor
selectivity. _Nat Rev Drug Discov_ 11, 21 (2012). https://doi.org/10.1038/nrd3647 Download citation * Published: 03 January 2012 * Issue Date: January 2012 * DOI:
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