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PROTACs in Epigenetic Cancer Therapy: Current Status and Future Opportunities

Xuelian Liu1,2,3, Anjin Wang1,2,3, Yuying Shi1,2,3

  • 1Department of Gynecological Oncology, Zhongnan Hospital of Wuhan University, Wuhan 430071, China.

Molecules (Basel, Switzerland)
|February 11, 2023
PubMed

Insights

Proteolytic targeted chimeras (PROTACs) offer a novel approach to degrade cancer-driving epigenetic proteins. This review explores PROTAC development for epigenetic cancer therapy, aiming to overcome drug resistance and advance treatment strategies.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Epigenetic dysregulation is a key driver of cancer development and progression.
  • Targeting the cancer epigenome offers promising therapeutic strategies, including overcoming drug resistance.
  • Proteolytic targeted chimeras (PROTACs) are an emerging modality for targeted protein degradation.

Purpose of the Study:

  • To review the progress of PROTAC degraders and drugs targeting epigenetic proteins in cancer.
  • To highlight the potential of PROTACs in epigenetic cancer therapy.
  • To discuss current challenges and future opportunities in this field.

Main Methods:

  • Literature review of PROTAC development in epigenetic cancer therapy.
  • Analysis of PROTACs targeting epigenetic regulators.
  • Discussion of mechanistic insights and therapeutic applications.

Main Results:

  • Numerous PROTAC degraders targeting epigenetic proteins have been designed.
  • PROTACs show promise in exploiting target druggability for epigenetic cancer therapy.
  • Targeting epigenetic proteins with PROTACs can enhance mechanistic understanding of cancer epigenetics.

Conclusions:

  • PROTACs represent a significant advancement in targeting epigenetic mechanisms in cancer.
  • Further development of PROTACs holds potential for novel cancer treatments and overcoming resistance.
  • Continued research is crucial to address challenges and unlock future opportunities for PROTACs in oncology.
Keywords:
PROTACscancer therapyepigeneticsprotein degradation

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