Literature review: A review to cross the hurdle of drug discovery with PROTACs

Posted: 22 September 2020 | | No comments yet

This review highlights five recent publications about homogeneous assays applied to PROTACs, a chemical knockdown approach for cancer research.

Where traditional drugs can target only around 20 percent of the proteome, a new technology called PROteolysis TArgeting Chimeras (PROTACs) could reach the other 80 percent, currently undruggable. This molecule promotes protein of interest ubiquitination by forming a ternary complex with an E3 ligase.

Like any new approach a lot of effort is necessary to develop the ternary complex with the best affinity. It has been found that homogeneous assays like HTRF or AlphaLISA are well suited to reaching this goal.