Targeted Protein Degradation Platform
About us
argeted Protein Degradation Platform (PROTACs):https://www.bocsci.com/targeted-protein-degradation-platform-protacs.html
An effective approach in drug discovery to access difficult diseases is Targeted Protein Degradation (TPD). TPD refers to the use of hetero-bifunctional small molecule "degraders" (e.g. PROTACs™) to achieve knockdown of target proteins within cells. Since its initial design by Sakamoto et al. in 2001, proteolysis-targeting chimera (PROTAC) technology has been successfully applied in the development of hetero-bifunctional molecules that can prompt target protein degradation. These hetero-bifunctional molecules generally consist of binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker. The binding of both moieties results in the formation of a ternary complex between target protein and E3 ligase, leading to polyubiquitination of the target protein, its recognition by the proteasome and subsequent degradation. By removing target proteins directly rather than merely blocking them, protein degraders may provide multiple advantages over small molecule inhibitors. While traditional drugs may only allow access to ~20% of the proteome, TPD techniques may open the door to the other 80%.