Related Experiment Video

Updated: Jun 29, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
06:07

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

Published on: August 5, 2022

2.6K

Therapeutic targeting of DNA methylation alterations in cancer

Abigail V Lee1, Kevin A Nestler1, Katherine B Chiappinelli1

  • 1Department of Microbiology, Immunology, & Tropical Medicine, The George Washington University, Washington, DC, USA.

Pharmacology & Therapeutics
|April 3, 2024
PubMed

Insights

Aberrant DNA methylation drives cancer by silencing genes and suppressing immunity. Inhibiting DNA methylation offers a promising therapeutic strategy to reactivate tumor suppressors and enhance antitumor responses.

Area of Science:

  • Epigenetics
  • Cancer Biology
  • Immunology

Background:

  • DNA methylation is crucial for gene regulation and cancer development.
  • Aberrant DNA methylation promotes uncontrolled cell growth and immune evasion.
  • Dysregulated DNA methylation is a hallmark of many cancers.

Purpose of the Study:

  • To elucidate the role of aberrant DNA methylation in cancer.
  • To describe mechanisms of tumorigenesis and immune modulation by DNA methylation.
  • To review therapeutic strategies targeting DNA methylation in cancer.

Main Methods:

  • Review of existing literature on DNA methylation in cancer.
  • Analysis of molecular mechanisms linking DNA methylation to cancer progression.
  • Examination of preclinical and clinical studies of DNA methylation inhibitors.

Main Results:

  • Hypermethylation of tumor suppressors and silencing of DNA repair genes contribute to cancer.
  • Aberrant DNA methylation impairs antitumor immune responses.
  • Pharmacologic inhibition of DNA methylation can restore gene expression and enhance immunity.

Conclusions:

  • Targeting DNA methylation is a viable cancer therapeutic strategy.
  • Combination therapies involving DNA methylation inhibitors show promise for enhancing antitumor immunity.
  • Further research is needed to optimize DNA methylation-targeted cancer treatments.
Keywords:
CancerDNA methylationDNMT inhibitor, epigenetic

More Related Videos

Genome-Wide Analysis of DNA Methylation in Gastrointestinal Cancer07:50

Genome-Wide Analysis of DNA Methylation in Gastrointestinal Cancer

Published on: September 18, 2020

5.5K
Enhanced Reduced Representation Bisulfite Sequencing for Assessment of DNA Methylation at Base Pair Resolution13:47

Enhanced Reduced Representation Bisulfite Sequencing for Assessment of DNA Methylation at Base Pair Resolution

Published on: February 24, 2015

25.5K

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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.
There are several types of targeted therapies against...
7.6K
Epigenetic Regulation01:37

Epigenetic Regulation

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...
3.0K
Phase II Reactions: Methylation Reactions01:17

Phase II Reactions: Methylation Reactions

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...
186
Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
3.3K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
4.9K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
6.5K