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Progress of proteolysis-targeting chimeras (PROTACs) delivery system in tumor treatment

Lianlian Fan1, Weifang Tong2, Anhui Wei3

  • 1Department of Pharmacy, China-Japan Union Hospital of Jilin University, Changchun 130033, China.

International Journal of Biological Macromolecules
|July 6, 2024
PubMed

Insights

Proteolysis targeting chimeras (PROTACs) offer a novel approach to degrade disease-causing proteins. Enhancing PROTAC delivery systems is crucial for overcoming challenges and advancing cancer treatment strategies.

Area of Science:

  • Oncology
  • Pharmacology
  • Biotechnology

Background:

  • Proteolysis targeting chimeras (PROTACs) leverage cellular machinery for targeted protein degradation, representing a promising strategy for cancer therapy.
  • Current limitations of PROTACs include poor solubility, low cell permeability, and off-target effects, hindering preclinical progression.
  • Effective delivery systems are essential to overcome these challenges and enable precise tumor targeting.

Purpose of the Study:

  • To systematically review the design principles of PROTAC delivery systems.
  • To summarize recent advancements in various PROTAC delivery strategies.
  • To propose constructive approaches for developing multifunctional PROTAC delivery systems.

Main Methods:

  • Literature review focusing on PROTAC delivery systems.
  • Analysis of design principles and recent advances.
  • Synthesis of strategies for multifunctional delivery systems.

Main Results:

  • Detailed overview of diverse PROTAC delivery system designs.
  • Identification of key challenges and their corresponding solutions.
  • Framework for developing advanced, multifunctional delivery systems.

Conclusions:

  • Multifunctional delivery systems are critical for the success of PROTACs in cancer therapy.
  • Further development of these systems will enhance PROTAC efficacy and safety.
  • This review provides insights to accelerate PROTAC drug development.
Keywords:
CereblonDelivery systemsE3 ubiquitin ligasePROTACProteolysis targeting chimerasVon Hippel-Lindau

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