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Synthesis of new PROTACs

PROteolysis Targeting Chimeras (PROTACs) are bifunctional molecules consisting of a ligand for the target Protein of Interest (POI) and a ligand for an E3 ubiquitin ligase: these ligands are covalently joined by a flexible linker. In cells, their mode of action is the following: recruitment of the E3 ligase in close proximity to the POI, ubiquitination of the POI, recognition and degradation of the POI by the Ubiquitin Proteasome System (UPS).
In other words, PROTACs hijack the native cellular degradation mechanism to selectively remove the POI from the cell.
At BioCIS, we work on the design, synthesis and biological evaluation of PROTACs targeting proteins that upregulate oncogenes or proliferation-promoting factors and inhibit tumor suppressors or proliferation restraining factors. The intentional and controlled degradation of these proteins could significantly inhibit tumorigenesis and represent a therapeutical strategy to treat cancer.