An overview of PROTACs: a promising drug discovery paradigm
Sichuan University · State Key Laboratory of Biotherapy · +1 more institution
Abstract
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target proteins by hijacking the ubiquitin-proteasome system. Currently, about 20-25% of all protein targets are being studied, and most works focus on their enzymatic functions. Unlike small molecules, PROTACs inhibit the whole biological function of the target protein by binding to the target protein and inducing subsequent proteasomal degradation. PROTACs compensate for limitations that transcription factors, nuclear proteins, and other scaffolding proteins are difficult to handle with traditional small-molecule inhibitors. Currently, PROTACs…
Citation impact
- FWCI
- 22.61
- Percentile
- 100%
- References
- 219
Authors
11Topics & keywords
- Drug discovery
- Computational biology
- Biology
- Bioinformatics
Funding
- NNNational Natural Science Foundation of ChinaAwards: 22007070, 22277086
- DODepartment of Science and Technology of Sichuan ProvinceAwards: 2022ZDZX0028, 2022NSFSC1409
- SUSichuan UniversityAwards: 2021HXBH006, ZYJC21075
- SPSichuan Province Science and Technology Support ProgramAwards: 2022NSFSC1409, 2022ZDZX0028
- WCWest China Hospital, Sichuan UniversityAwards: ZYJC21075, 2021HXBH006, 1.3.5