Targeted protein degradation: elements of PROTAC design.

@article{Paiva2019TargetedPD,
  title={Targeted protein degradation: elements of PROTAC design.},
  author={Stacey-Lynn Paiva and C. Crews},
  journal={Current opinion in chemical biology},
  year={2019},
  volume={50},
  pages={
          111-119
        }
}
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the degradation of select proteins of interest (POIs) by hijacking the activity of E3 ubiquitin ligases for POI ubiquitination and subsequent degradation by the 26S proteasome. This hijacking mechanism has been used to degrade various types of disease-relevant POIs. In this review, we aim to highlight the recent advances in targeted protein… Expand
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References

SHOWING 1-10 OF 115 REFERENCES
Targeted protein degradation and the enzymology of degraders.
PROTAC-mediated crosstalk between E3 ligases.
Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation
Delineating the role of cooperativity in the design of potent PROTACs for BTK
...
1
2
3
4
5
...