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PROTACs in gastrointestinal cancers

Yu Chen1,2, Qingfan Yang3, Jinrun Xu1,2

  • 1Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646000, China.

Molecular Therapy Oncolytics
|November 24, 2022
PubMed

Insights

Proteolysis targeting chimeras (PROTACs) offer a novel method for targeted protein degradation, showing promise in treating gastrointestinal cancers. This technology is advancing rapidly, with 15 PROTACs in clinical trials for various targets.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules designed for targeted protein degradation (TPD).
  • PROTACs leverage the ubiquitin-proteasome system (UPS) to selectively degrade target proteins.
  • This technology offers advantages such as broad targeting, cell permeability, tissue specificity, and oral bioavailability.

Purpose of the Study:

  • To review the mechanism, research progress, and clinical applications of PROTACs.
  • To summarize achievements in developing PROTACs for gastrointestinal cancers.
  • To discuss the benefits and challenges of PROTACs in cancer therapy.

Main Methods:

  • Literature review of PROTAC technology and its applications.
  • Analysis of PROTAC development for gastrointestinal cancer targets.
  • Examination of ongoing clinical trials involving PROTACs.

Main Results:

  • PROTACs have demonstrated significant potential in targeted protein degradation.
  • Numerous PROTACs targeting gastrointestinal cancers have been developed, with validated targets.
  • Fifteen PROTACs are currently in clinical trials, indicating rapid advancement.

Conclusions:

  • PROTAC technology represents a powerful strategy for targeted protein degradation in cancer treatment.
  • The application of PROTACs in gastrointestinal cancers is a rapidly evolving field with promising clinical outcomes.
  • Further research and development are crucial to overcome challenges and maximize the therapeutic potential of PROTACs.
Keywords:
E3 ligasesPROTACscancer treatmentgastrointestinal cancerstargeted protein degradation

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