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Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
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PROTACs: Promising Approaches for Epigenetic Strategies to Overcome Drug Resistance

Sarah F Giardina1, Elena Valdambrini1, J David Warren2

  • 1Department of Microbiology and Immunology, Weill Cornell Medicine, 1300 York Ave, Box 62, New York, NY, United States.

Current Cancer Drug Targets
|February 4, 2021
PubMed

Insights

Epigenetic alterations drive cancer development and therapy resistance. Novel Proteolysis Targeting Chimera (PROTAC) strategies offer new ways to target the epigenome and overcome drug resistance in cancer treatment.

Area of Science:

  • Molecular Biology
  • Cancer Research
  • Epigenetics

Background:

  • Epigenetic modifications, including DNA methylation and histone modifications, regulate gene expression crucial for tissue development.
  • Dysregulation of epigenetic processes contributes to cancer initiation and progression by altering cellular signaling pathways.
  • Epigenetic therapies show promise for hematological malignancies, but cancer cells develop resistance through population heterogeneity.

Purpose of the Study:

  • To explore novel drug discovery approaches targeting the cancer epigenome.
  • To address the challenge of therapy resistance in cancer treatment.
  • To highlight the potential of Proteolysis Targeting Chimeras (PROTACs) in epigenome-targeted drug development.

Main Methods:

  • Review of recent advancements in understanding epigenetic mechanisms in cancer.
  • Analysis of current epigenetic therapies and clinical trials.
  • Exploration of Proteolysis Targeting Chimera (PROTAC) technology for targeted protein degradation.

Main Results:

  • Epigenetic dysregulation is a key factor in cancer development and heterogeneity.
  • Cancer cells develop resistance to epigenetic therapies through dynamic survival strategies.
  • PROTACs represent a promising novel approach for targeting the epigenome and overcoming drug resistance.

Conclusions:

  • Targeting the epigenome is critical for effective cancer treatment.
  • Proteolysis Targeting Chimeras (PROTACs) offer a new avenue for developing drugs against resistant cancers.
  • Further research into PROTACs is warranted to combat cancer's adaptive resistance mechanisms.
Keywords:
CancerPROTACdrug resistanceepigeneticsoncologytherapy resistance

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