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Methods Mol Biol. 2011;779:185-97. doi: 10.1007/978-1-61779-264-9_10.

Sensitizing plant protein kinases to specific inhibition by ATP-competitive molecules.

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Department of Plant Sciences, Tel-Aviv University, Tel-Aviv, Israel.


The highly conserved nature of the protein kinase catalytic domain and the low permeability of plant cell membranes pose a challenge to the development of specific inhibitors that target individual protein kinases in vivo. Here, we describe a chemical-genetic approach to specifically sensitize individual plant kinases to cell-permeable small molecules that do not inhibit wild-type kinases. In this approach, a single amino-acid substitution is introduced in the ATP-binding site of the enzyme enabling specific binding of ATP-competitive molecules. Cell-permeable molecules can then be used to specifically target the sensitized allele in transgenic Arabidopsis thaliana plants that do not express the wild-type form of the kinase. This strategy provides a useful tool for the functional characterization of protein kinases in planta and for the dissection of the signaling pathways in which they are involved.

[Indexed for MEDLINE]

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