Article
Chemical genetic strategy for targeting protein kinases based on covalent complementarity.
Proceedings of the National Academy of Sciences of the United States of America - 13 Sept 2011
Garske Adam L, Peters Ulf, Cortesi Arianna T, Perez Jenny L, Shokat Kevan M
Abstract excerpt
The conserved nature of the ATP-binding site of the > 500 human kinases renders the development of specific inhibitors a challenging task. A widely used chemical genetic strategy to overcome the specificity challenge exploits a large-to-small mutation of the gatekeeper residue (a conserved hydrophobic amino acid) and the use of a bulky inhibitor to achieve specificity via shape complementarity. However, in a...
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