Targeting protein-protein interactions (PPIs) using non-peptide small-molecules has been traditionally difficult and is an under-explored area for new therapeutic discovery. In this presentation, I will talk about several approaches we have employed in our laboratory for the discovery and optimization of highly potent, specific and orally bioavailable small-molecule inhibitors targeting several different PPIs. A number of these small-molecule inhibitors are now in clinical development for the treatment of different types of human cancers.

Targeting protein-protein interactions for new cancer therapeutics

249th National Meeting (2015)

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