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Recent Advances in Small Molecule PROTACs for the Treatment of Cancer

Wen Li1, Reham M Elhassan1, Xuben Hou1

  • 1Department of Medicinal Chemistry and Key Laboratory of Chemical Biology of Natural Products (MOE), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China.

Current Medicinal Chemistry
|November 19, 2020
PubMed

Insights

PROTACs offer targeted protein degradation for cancer therapy, showing advantages over traditional inhibitors. This review covers PROTAC technology, its benefits, and recent advancements in small-molecule PROTACs for cancer treatment.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • PROTACs (PROteolysis TArgeting Chimeras) leverage the ubiquitin-proteasome system for targeted protein degradation.
  • This approach is emerging as a promising strategy in targeted cancer therapy.

Purpose of the Study:

  • To introduce the mechanism, characteristics, and advantages of PROTAC technology.
  • To summarize recent advancements in small-molecule PROTAC development for cancer treatment.

Main Methods:

  • Review of existing literature on PROTAC technology.
  • Analysis of PROTACs' pharmacodynamics, selectivity, and drug resistance profiles.
  • Summary of clinical trial progress for small molecule PROTACs.

Main Results:

  • PROTACs demonstrate significant advantages over traditional small-molecule inhibitors.
  • Several small molecule PROTACs are currently in Phase I clinical trials.
  • PROTACs offer improved pharmacodynamics, selectivity, and ability to overcome drug resistance.

Conclusions:

  • PROTAC technology presents a viable alternative to conventional cancer therapies.
  • Further optimization in small-molecule PROTAC design is crucial for advancing targeted anticancer research.
Keywords:
AnticancerE3 ligasePROTACligandprotein degradationtransduction.ubiquitination

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