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Molecular Processes Exploited as Drug Targets for Cancer Chemotherapy

Satya P Gupta1, Anjana Sharma1, Vaishali M Patil2

  • 1Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut-250005, India.

Anti-Cancer Agents in Medicinal Chemistry
|November 19, 2020
PubMed

Insights

Epigenetics, including DNA methylation and histone modification, significantly contributes to cancer development. Targeting these epigenetic regulators offers promising therapeutic strategies for various cancers, despite associated challenges.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Cancer is characterized by uncontrolled malignant cell growth and significant molecular diversity, complicating treatment selection.
  • Cancer development involves a complex series of molecular events, prompting research into underlying processes.
  • Epigenetic mechanisms, specifically DNA methylation and histone modification, are increasingly recognized as critical contributors to oncogenesis.

Purpose of the Study:

  • To provide an overview of epigenetics in cancer, focusing on DNA methylation and histone modification.
  • To explore the potential of targeting epigenetic regulators as a therapeutic strategy for cancer treatment.
  • To summarize FDA-approved drugs targeting epigenetic enzymes and discuss challenges in developing epigenetic-based cancer therapeutics.

Main Methods:

  • Literature review focusing on epigenetic mechanisms in cancer.
  • Analysis of DNA methylation and histone modification pathways involved in tumorigenesis.
  • Summary of current FDA-approved drugs targeting epigenetic regulators in clinical use.

Main Results:

  • Epigenetic alterations, including aberrant DNA methylation and histone modifications, are hallmarks of cancer.
  • Targeting enzymes involved in DNA methylation and histone modification has shown efficacy in preclinical and clinical settings for various cancers.
  • Several FDA-approved drugs targeting epigenetic regulators are available, demonstrating the clinical relevance of this approach.

Conclusions:

  • Epigenetics plays a crucial role in cancer initiation and progression, making epigenetic regulators attractive therapeutic targets.
  • Targeted epigenetic therapies offer a promising avenue for cancer treatment, with ongoing research addressing challenges in drug development and patient selection.
  • Understanding the interplay of epigenetic modifications is vital for advancing precision oncology and developing more effective anti-cancer strategies.
Keywords:
CancerDNA methylationchemotherapyepigeneticshistone modificationmolecular therapeutics.

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