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Novel Technologies in PROTAC Design

  • Keerti Jain,
  • Sukuru Chinna Reddy,
  • Sreevardhan Moode,
  • Piyush Mehra,
  • Sofiya Tarannum,
  • Manisha Patel,
  • Vineet Kumar Jain,
  • Harvinder Popli

摘要

Proteolysis Targeting Chimeras (PROTACs) mediated degradation of targeted protein or protein of interest (POI) is emerging as a fascinating approach for drug discovery and exploring new therapeutic modalities. PROTACs work by hijacking the activity of E3 ubiquitin ligases responsible for ubiquitination of POI, which subsequently leads to degradation of POI by 26S proteasome. This hijacking mechanism of PROTACs is being explored to degrade different POIs involved in various types of diseases. In this chapter, we have discussed different technologies being explored for the design of efficient and potent PROTACs for various severe and critical disorders including cancer.