Allosteric Inhibition of the Protein-Protein Interaction Between the Leukemia-Associated Proteins RUNX1 and CBFβ.
Chemistry & Biology 2007; 14(10):1186-1197.

Numerous inhibitors of enzymatic activity have been developed, however the development of inhibitors of protein-protein interactions has only recently come to the forefront as a viable approach. Allosteric inhibition of such protein-protein interactions presents a number of advantages, including not having to compete for binding with the partner protein, however to date there are very few examples of such inhibitors. We have developed novel allosteric small molecule inhibitors of the binding of RUNX1 to CBFβ, two proteins whose translocations play a critical role in the development of acute myeloid leukemia and acute lymphocytic leukemia.

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