Strategies that selectively bind proteins of interest and target them to the intracellular protein recycling machinery for targeted protein degradation have recently emerged as powerful tools for undruggable targets in biomedical research and the pharmac
Targeted protein degradation via intramolecular bivalent glues. Nature 627, 204–211 (2024). Article CAS PubMed PubMed Central Google Scholar Kerres, N. et al. Chemically induced degradation of the oncogenic transcription factor BCL6. Cell Rep. 20, 2860–2875 (2017). Article CAS PubMed ...
Conjugation of this macrocycle to a potent BRD4 ligand enabled generation of chimeric molecules that effectively degrade BRD4 in cells, thus demonstrating that degradation via direct proteasomal recruitment is a viable strategy for targeted protein degradation....
Targeted Protein Degradation (TPD) is a method that uses small molecule "Degraders", such as PROTAC®Degraders, SNIPERS and molecular glues, to achieve knockdown of target proteins within cells. Degraders form a ternary complex with both the protein of interest and an E3 ligase. This induced ...
Targeted protein degradation (TPD) is a drug discovery method that removes harmful proteins by using PROTACs®, which bring a target protein and an enzyme together for degradation by the proteasome.
Targeted protein degradation is arguably one of the most exciting novel therapeutic modalities in drug discovery. Moving away from occupancy-based pharmacology models and their challenges with selectivity, on/off target toxicities, and PK–PD limitations, it provides a novel and orthogonal therapeutic pa...
Explore targeted protein degradation approaches with BPS Bioscience. Discover innovative strategies and applications for selectively eliminating proteins to advance research and therapeutic development.
Neklesa TK, Winkler JD, Crews CM. Targeted protein degradation by PROTACs. Pharmacol Ther. 2017;174:138-144.Neklesa, T.K.; Winkler, J.D.; Crews, C.M. Targeted protein degradation by PROTACs. Pharmacol. Ther. 2017. [CrossRef] [PubMed]...
Targeted protein degradation assays to rapidly screen small molecules that trigger protein degradation, & to quantify endogenous protein turnover.
靶向蛋白降解(Targeted protein degradation, TPD)在过去二十年中作为一种主要的新型药物模式已被广泛用于多种蛋白,为癌症、炎症等疾病治疗提供了一种潜在的有前途的治疗策略。 其中,蛋白降解靶向嵌合体(Proteolysis targeting chimeras,PROTAC)作为一种有潜力的靶向蛋白降解技术,它是具有E3泛素连接酶招募者与感兴趣蛋白(...