An emerging modality of therapeutics called PROteolysis TArgeting Chimeras (PROTACs) could enable the design of new drugs targeting “undruggable” proteins, which make up to 85% of the proteome. Their novel mode of action allows them to hijack a cells natural function and initiate degradation of the target protein for a particular disease. This development has led to great interest in the pharmaceutical and biotechnology industries. However, synthesis of PROTACs requires numerous evaporation steps, causing bottlenecks in their production and slowing the drug development process. This article introduces PROTACs and the benefits they can offer to the drug discovery field, before discussing how the issues with their synthesis can be overcome.



The mechanism of action of a PROTAC. The heterobifunctional molecule comprises of an E3 ligand (yellow oval), a chemical linker (blue bar) and ligand for the protein of interest (red triangle).


#PROTAC #drugdiscovery #evaporation #bottlenecks #AZoNetwork

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