Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 19, Issue 20, Pages 1784-1788Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026619666191011162955
Keywords
PROTACs; ENDTAC; degradation; progress; challenges; UPS
Categories
Funding
- China Postdoctoral Science Foundation [2019M652586]
- Postdoctoral Research Grant in Henan Province [1902001, 19030008]
- Henan Medical Science and Technology Program [2018020601]
Ask authors/readers for more resources
Proteolysis targeting chimeras (PROTACs), as a novel therapeutic modality, play a vital role in drug discovery. Each PROTAC contains three key parts; a protein-of-interest (POI) ligand, a E3 ligase ligand, and a linker. These bifunctional molecules could mediate the degradation of POIs by hijacking the activity of E3 ubiquitin ligases for POI ubiquitination and subsequent degradation via the ubiquitin proteasome system (UPS). With several advantages over other therapeutic strategies, PROTACs have set off a new upsurge of drug discovery in recent years. ENDTAC, as the development of PROTACs technology, is now receiving more attention. In this review, we aim to summarize the rapid progress from 2018 to 2019 in protein degradation and analyze the challenges and future direction that need to be addressed in order to efficiently develop potent protein degradation technology.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available