PROTAC technology: From drug development to probe technology for target deconvolution.

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  • Additional Information
    • Source:
      Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE
    • Publication Information:
      Publication: Paris : Editions Scientifiques Elsevier
      Original Publication: Paris, S.E.C.T. [etc.]
    • Subject Terms:
      Drug Discovery* ; Drug Development*; Humans ; Ubiquitin-Protein Ligases/metabolism ; Ubiquitin-Protein Ligases/antagonists & inhibitors ; Ligands ; Molecular Structure
    • Abstract:
      Drug development remains a critical focus within the global pharmaceutical industry. To date, more than 80 % of disease targets are considered difficult to target. The emergence of PROTAC technology has, to some extent, alleviated this challenge. Since introduction, PROTAC technology has evolved through the peptide E3 ligase ligand phase and the small molecule E3 ligase ligand phase. Currently, multiple PROTAC molecules are in the clinical research phase, showing promising potential for addressing drug resistance, disease recurrence, and intractable targets. Target deconvolution is a crucial step in the drug discovery and development process. Due to the exceptional targeting ability and specificity of PROTAC, it is widely used and promoted as an innovative technology for discovering new drug targets, leading to significant breakthroughs. The use of PROTAC probe requires only a catalytic dose and weak interaction with the target protein to achieve target degradation. Thus, it offers substantial advantages over traditional probes, particularly in identifying new targets that are low-abundance or difficult to target. This review provides a comprehensive overview of the advancements made by PROTAC technology in drug development and drug target discovery, while also systematically reviewing the workflow of PROTAC probe. With the ongoing development of PROTAC technology, PROTAC probe is poised to become a key research area in future drug target deconvolution.
      Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
      (Copyright © 2024 Elsevier Masson SAS. All rights reserved.)
    • Contributed Indexing:
      Keywords: Drug development; PROTAC; PROTAC probe; Pro-PROTAC; Target deconvolution
    • Accession Number:
      EC 2.3.2.27 (Ubiquitin-Protein Ligases)
      0 (Ligands)
    • Publication Date:
      Date Created: 20240731 Date Completed: 20240809 Latest Revision: 20240813
    • Publication Date:
      20240813
    • Accession Number:
      10.1016/j.ejmech.2024.116725
    • Accession Number:
      39083982