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Related Concept Videos

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.
The mechanism of methylation unfolds in two stages. The first stage sees a methyltransferase enzyme facilitating the transfer of a methyl group from S-adenosylmethionine (SAM) to the substrate, forming S-adenosylhomocysteine (SAH). The second stage involves further metabolism of SAH into homocysteine, which can be recycled...
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Epigenetic Regulation01:37

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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.
X-chromosome...
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Epigenetic Regulation01:46

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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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Related Experiment Video

Updated: Apr 20, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
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Targeting DNA methylation with small molecules: what's next?

Alexandre Erdmann1, Ludovic Halby1, Jacques Fahy1

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DNA methylation, an epigenetic mark regulating gene expression, is crucial in cancer. New non-nucleoside inhibitors are being developed to target this process, offering potential therapeutic strategies for cancer treatment.

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Area of Science:

  • Epigenetics
  • Molecular Biology
  • Cancer Research

Background:

  • DNA methylation is a key epigenetic mechanism controlling gene expression in mammals.
  • Aberrant DNA methylation patterns are implicated in various diseases, particularly cancer, by silencing tumor suppressor genes.
  • The reversibility of DNA methylation makes it a druggable target, with existing approved therapies for hematological cancers.

Purpose of the Study:

  • To review current efforts in discovering novel molecules that inhibit DNA methylation in cancer cells.
  • To focus on non-nucleoside inhibitors and their mechanisms.
  • To define the characteristics of an ideal DNA methylation inhibitor for cancer therapy.

Main Methods:

  • Literature review of non-nucleoside inhibitors targeting DNA methylation.
  • Analysis of the role of DNA methylation in cancer.
  • Discussion of the features of effective DNA methylation inhibitors.

Main Results:

  • DNA methylation plays a dual role in cancer: silencing protective genes and activating harmful elements.
  • Several non-nucleoside compounds are under investigation for their potential to inhibit DNA methylation.
  • Understanding inhibitor features is crucial for developing new cancer treatments.

Conclusions:

  • Non-nucleoside inhibitors represent a promising avenue for developing novel epigenetic therapies against cancer.
  • Further research is needed to identify and optimize inhibitors with ideal characteristics for clinical application.
  • Targeting DNA methylation offers a viable strategy for cancer treatment, building on existing successes.