Abstract:

Protein-protein interactions (PPIs) represent a large class of under-explored therapeutic targets and targeting PPIs has traditionally been considered as “undruggable”. Our laboratory has been focusing on developing small-molecules to block PPIs as a novel therapeutic strategy for the development of new cancer medicines. Our efforts have led to advancement of 10 compounds currently in Phase 1-3 clinical development and several more in advanced preclinical development. In this lecture, I will share with you our journey in targeting PPIs, using both inhibition and degradation strategies. Our research has demonstrated that many PPIs are druggable targets and targeting PPIs represents a promising therapeutic strategy for cancer and other human diseases.