Correlation Engine 2.0
Clear Search sequence regions


  • chimeras (5)
  • humans (1)
  • libraries (2)
  • proteolysis (5)
  • Sizes of these terms reflect their relevance to your search.

    Targeted protein degradation by small-molecule degraders represents an emerging mode of action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules that can recruit an E3 ligase and a protein of interest (POI) into proximity, leading to induced ubiquitination and degradation of the POI by the proteasome system. To date, the design and optimization of PROTACs remain empirical due to the complicated mechanism of induced protein degradation. Nevertheless, it is increasingly appreciated that profiling step-by-step along the ubiquitin-proteasome degradation pathway using biochemical and biophysical assays are essential in understanding the structure-activity relationship and facilitating the rational design of PROTACs. This review aims to summarize these assays and to discuss the potential of expanding the toolbox with other new techniques.

    Citation

    Xingui Liu, Xuan Zhang, Dongwen Lv, Yaxia Yuan, Guangrong Zheng, Daohong Zhou. Assays and technologies for developing proteolysis targeting chimera degraders. Future medicinal chemistry. 2020 Jun;12(12):1155-1179

    Expand section icon Mesh Tags

    Expand section icon Substances


    PMID: 32431173

    View Full Text