Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits target protein and E3 ubiquitin ligase together to trigger proteasomal degradation of target protein by the ubiquitin-proteasome system. PROTAC has emerged as a promising approach for targeted therapy in various diseases, particularly in cancers. In this review, we introduce the principle and development of PROTAC technology, as well as the advantages of PROTACs over traditional anti-cancer therapies. Moreover, we summarize the application of PROTACs in targeting critical oncoproteins, provide the guidelines for the molecular design of…

• NN
  National Natural Science Foundation of China

  Awards: 81821002, 81772960, 82073319
• DO
  Department of Science and Technology of Sichuan Province

  Award: 2019JDTD0013
• SU
  Sichuan University

  Awards: ZYGD20008, ZYJC18030
• WC
  West China Hospital, Sichuan University

  Awards: ZYJC18030, ZYGD20008, 1.3.5