Clinical Translation of Targeted Protein Degraders

The document discusses the emerging field of targeted protein degradation (TPD) as a promising therapeutic approach, particularly in cancer treatment. It highlights the use of molecular glue degraders and heterobifunctional proteolysis targeting chimeras (PROTACs) to target proteins previously considered undruggable. These degraders work by inducing interactions with E3 ligases, leading to the degradation of proteins-of-interest (POIs) through the ubiquitin-proteasome system. The review notes a significant increase in degraders entering clinical trials, with most utilizing the CRL4CRBN E3 ligase and targeting a limited range of POIs. The authors provide insights into the development of these degraders and emerging human data, which are valuable for researchers in the TPD field.