Related Experiment Video

Updated: May 23, 2026

The Development and Application of Biophysical Assays for Evaluating Ternary Complex Formation Induced by Proteolysis Targeting Chimeras (PROTACS)
07:22

The Development and Application of Biophysical Assays for Evaluating Ternary Complex Formation Induced by Proteolysis Targeting Chimeras (PROTACS)

Published on: January 12, 2024

Proteolysis-targeting chimera (PROTAC) in cancer: design principles and applications on "undruggable" targets

Xun Lu1,2,3, Jianliang Qin4, Shuilin Dong1,2,3

  • 1Division of Hepato-Pancreato-Biliary Surgery, Tongji Hospital, Tongji Medical College, Huazhong University of Science & Technology, 1095 Jiefang Avenue, Wuhan, 430030, China.

Biomarker Research
|May 22, 2026
PubMed

Insights

Proteolysis-targeting chimeras (PROTACs) offer a novel approach to target previously "undruggable" cancer proteins. This review details PROTAC design, delivery, and its potential to expand cancer therapy options.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Targeted cancer therapies aim to improve efficacy and reduce side effects by modulating biomolecule distribution.
  • Many critical cancer-related proteins remain

Purpose of the Study:

  • To provide a comprehensive overview of proteolysis-targeting chimeras (PROTACs) for targeting
  • To discuss the design principles of PROTACs, including ligands, linkers, and ternary complex prediction.
  • To review the application of PROTACs against challenging

Main Methods:

  • Detailed elaboration on the design of protein of interest (POI) ligands, E3 ligase ligands, and linkers.
  • Prediction of PROTAC ternary complex structures.
  • Review of PROTAC delivery systems and carrier utilization.

Main Results:

  • Discussion on the current status of PROTACs targeting key
  • Analysis of the advantages and disadvantages of PROTAC delivery systems.
  • Exploration of PROTACs' potential in overcoming resistance mechanisms.

Conclusions:

  • PROTACs represent a promising strategy for targeting previously undruggable proteins in cancer therapy.
  • Further research into PROTAC design and delivery systems is crucial for clinical translation.
  • PROTAC technology has the potential to significantly broaden the scope of therapeutic targets in oncology.
Keywords:
Applications on “undruggable” targetsDesign principlesProteolysis-targeting chimera (PROTAC)

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