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Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Phase II Reactions: Methylation Reactions01:17

Phase II Reactions: Methylation Reactions

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Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
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Epigenetic Regulation01:37

Epigenetic Regulation

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Epigenetic changes alter the physical structure of the DNA without changing the genetic sequence and often regulate whether genes are turned on or off. This regulation ensures that each cell produces only proteins necessary for its function. For example, proteins that promote bone growth are not produced in muscle cells. Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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Pharmacogenomics: Identification of New Drug Targets01:29

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Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
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Related Experiment Video

Updated: Feb 22, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
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Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors

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DNA Methylation-Targeted Drugs.

Elodie M Da Costa1, Gabrielle McInnes, Annie Beaudry

  • 1From the Département de Pharmacologie et de Physiologie, Université de Montréal and Sainte-Justine University Hospital Research Center, Montréal, Québec, Canada.

Cancer Journal (Sudbury, Mass.)
|September 20, 2017
PubMed
Summary
This summary is machine-generated.

DNA methyltransferase inhibitors reprogram cancer cell epigenomes, offering a new avenue for cancer treatment. Further research into these epigenetic drugs may improve efficacy and overcome resistance in various cancers.

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Targeted DNA Methylation Analysis by Next-generation Sequencing
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Enhanced Reduced Representation Bisulfite Sequencing for Assessment of DNA Methylation at Base Pair Resolution
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Area of Science:

  • Epigenetics
  • Cancer Biology
  • Pharmacology

Background:

  • DNA hypermethylation is a hallmark of cancer, driving uncontrolled cell proliferation.
  • Approved DNA methyltransferase inhibitors (DNMTis) are effective against hematologic malignancies.
  • Drug resistance and limited efficacy in solid tumors necessitate novel therapeutic strategies.

Purpose of the Study:

  • To review the role of DNA methyltransferase inhibitors in cancer therapy.
  • To highlight the development of second-generation DNMTis.
  • To explore the potential of DNMTis in combination therapies for broader clinical application.

Main Methods:

  • Review of preclinical and clinical studies on DNA methyltransferase inhibitors.
  • Analysis of epigenetic reprogramming mechanisms by nucleoside analogs.
  • Evaluation of synergistic potential with chromatin-targeting agents and immunotherapy.

Main Results:

  • DNMTis reprogram cancer epigenomes, leading to reduced proliferation, increased differentiation, and enhanced immune recognition.
  • Second-generation DNMTis are in clinical trials to improve efficacy and overcome resistance.
  • DNMTis show promise in combination therapies for both hematologic and solid tumors.

Conclusions:

  • DNA methyltransferase inhibitors represent a promising epigenetic therapy for cancer.
  • Combination strategies involving DNMTis may overcome current treatment limitations.
  • Further clinical investigation is warranted to fully realize the therapeutic potential of DNMTis in diverse cancer types.