Harnessing the biology of the cell to target "undruggable" targets using PROTAC technology

【摘要】：For many years there have been certain intracellular targets which play a key role in cell signalling,molecular interactions and disease indications which have been termed"undruggable".This terminology has arisen as in many cases traditional approaches to develop small molecules that target these proteins have been unsuccessful.Proteolysis targeting chimera's(PROTAC technology) is one new mechanism which facilitates specific degradation of intracellular proteins by harnessing the ubiquitin proteasome system and E3ligase enzymes.This drives targeted ubiquitination and degradation of specific proteins in the cell as a new modality for therapeutic intervention.In this presentation I will cover the concept of PROTAC's and show some of the areas that AstraZeneca is exploring with this exciting technology.