Related Experiment Video

Updated: Jun 6, 2026

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
10:27

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts

Published on: July 25, 2020

Epigenetic cancer therapy: Proof of concept and remaining challenges

Cora Mund1, Frank Lyko

  • 1Global Drug Discovery, Research and Development, Bayer Schering Pharma, Berlin, Germany.

Bioessays : News and Reviews in Molecular, Cellular and Developmental Biology
|December 15, 2010
PubMed

Insights

Epigenetic cancer therapies show promise but lack specificity. Further research into targeted enzyme inhibition and pathway interactions is needed to establish clinical proof-of-concept for these epigenetic drugs.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Epigenetic modifications, including DNA methylation and histone alterations, are hallmarks of human cancers.
  • Epigenetic cancer therapy aims to reverse these aberrant patterns by inhibiting key enzymes.
  • Current epigenetic drugs exhibit limited specificity, hindering clinical validation.

Purpose of the Study:

  • To review the functional roles of major epigenetic modifier enzymes in cancer development.
  • To identify potential drug targets within epigenetic pathways.
  • To discuss strategies for enhancing the specificity of epigenetic cancer therapies.

Main Methods:

  • Literature review of DNA methyltransferases, histone deacetylases, histone methyltransferases, and demethylases.
  • Analysis of existing data on the role of these enzymes in cancer.
  • Synthesis of information regarding drug specificity and therapeutic potential.

Main Results:

  • DNA methyltransferases, histone deacetylases, histone methyltransferases, and demethylases play significant roles in cancer progression.
  • Several epigenetic modifier enzymes present viable targets for novel cancer therapies.
  • Lack of specificity in current drugs is a major challenge for clinical application.

Conclusions:

  • Clinical proof-of-concept for epigenetic cancer therapies is not yet established due to drug specificity issues.
  • Targeted inhibition of specific epigenetic enzymes is crucial for therapeutic success.
  • Exploring interactions between epigenetic pathways may improve cancer-specific targeting and treatment outcomes.

More Related Videos

An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues10:41

An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues

Published on: April 5, 2018

Epigenetic Engineering of K562 Cells: Dual-Vector Episomal Strategy for Stable Targeted DNA Methylation using dCas9-DNMT3A and -HDAC1 Fusion Proteins09:56

Epigenetic Engineering of K562 Cells: Dual-Vector Episomal Strategy for Stable Targeted DNA Methylation using dCas9-DNMT3A and -HDAC1 Fusion Proteins

Published on: October 31, 2025

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 specific...
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 specific...
Cancer Therapies02:49

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
Treatment Resistent Cancers02:56

Treatment Resistent 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...
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...
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...