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Related Concept Videos

Epigenetic Regulation01:46

Epigenetic Regulation

Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
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...
Epigenetic Regulation01:46

Epigenetic Regulation

Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
Histone Modification02:32

Histone Modification

The histone proteins have a flexible N-terminal tail extending out from the nucleosome. These histone tails are often subjected to post-translational modifications such as acetylation, methylation, phosphorylation, and ubiquitination. Particular combinations of these modifications form “histone codes” that influence the chromatin folding and tissue-specific gene expression.
Acetylation
The enzyme histone acetyltransferase adds acetyl group to the histones. Another enzyme, histone deacetylase,...
Histone Modification02:32

Histone Modification

The histone proteins have a flexible N-terminal tail extending out from the nucleosome. These histone tails are often subjected to post-translational modifications such as acetylation, methylation, phosphorylation, and ubiquitination. Particular combinations of these modifications form “histone codes” that influence the chromatin folding and tissue-specific gene expression.
Acetylation
The enzyme histone acetyltransferase adds acetyl group to the histones. Another enzyme, histone deacetylase,...
Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
These groups modify specific amino acids in a protein.

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Related Experiment Video

Updated: May 15, 2026

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
10:28

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers

Published on: September 20, 2018

Polyamine-based small molecule epigenetic modulators.

Shiv K Sharma1, Stuart Hazeldine, Michael L Crowley

  • 1Department of Pharmaceutical Sciences, Wayne State University, Detroit, MI, 48202, USA.

Medchemcomm
|January 8, 2013
PubMed
Summary
This summary is machine-generated.

New histone deacetylase (HDAC) and lysine-specific demethylase 1 (LSD1) inhibitors were developed. These epigenetic drugs re-express silenced cancer genes, offering a novel approach to cancer chemotherapy.

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Published on: June 25, 2018

Area of Science:

  • Epigenetics
  • Cancer Drug Discovery
  • Medicinal Chemistry

Background:

  • Histone deacetylases (HDACs) and lysine-specific demethylase 1 (LSD1) are validated targets in cancer drug discovery.
  • While several HDAC inhibitors exist, isoform-specific inhibitors are still needed.
  • Targeting histone demethylases is an emerging area in cancer research.

Purpose of the Study:

  • To design and synthesize novel inhibitors targeting HDACs and LSD1.
  • To evaluate the biological activity of these novel epigenetic modulators.
  • To explore their potential in cancer therapy, particularly in combination with agents like 5-azacytidine.

Main Methods:

  • Development of multiple series of small molecule inhibitors.
  • Chemical synthesis and characterization of novel analogues.
  • Biological evaluation of inhibitor efficacy in promoting gene re-expression.

Main Results:

  • Successful design and synthesis of novel HDAC and LSD1 inhibitor series.
  • Demonstrated ability of these compounds to re-express aberrantly silenced genes crucial in cancer.
  • Established the foundation for further development as cancer therapeutics.

Conclusions:

  • Novel HDAC and LSD1 inhibitors have been developed.
  • These compounds show potential for re-expressing silenced cancer genes.
  • This work contributes to the development of epigenetic-based cancer therapies.