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Curr Opin Chem Biol. 2009 Jun;13(3):284-90. doi: 10.1016/j.cbpa.2009.05.125. Epub 2009 Jun 22.

The road less traveled: modulating signal transduction enzymes by inhibiting their protein-protein interactions.

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  • 1Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, United States. michelle.arkin@ucsf.edu


The biological functions of intracellular signaling enzymes typically depend on multiple protein-protein interactions (PPI) with substrates, scaffolding proteins, and other cytoplasmic molecules. Blocking these interactions provides an alternative means to modulate signaling activity without fully ablating the catalytic activity of the target. Several recent reports describe small-molecule antagonists that target PPI sites on signaling enzymes. These findings suggest that such sites may often be druggable. However, the hypothesis that targeting such sites might confer on the resulting inhibitors improved properties of efficacy and/or tolerability, while appealing, remains largely untested.

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