PROteolysis TArgeting Chimeras – or PROTACs – are highly specific medicines that degrade unwanted or harmful proteins in cells. PROTACs are bifunctional molecules with two heads connected by a linker. One ‘head’ of the molecule selectively binds the target protein and a second ‘head’ of the molecule recruits a cellular enzyme, an E3 ubiquitin ligase. This enables the PROTAC to bring the ligase enzyme into close contact with the target protein, enabling the protein to be labelled with a ubiquitin tag and targeted for degradation by the ubiquitin-proteasome system. This process utilises the cell’s natural waste disposal system, resulting in the protein being eliminated from the cell.
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