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Related Concept Videos

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.
X-chromosome...
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Covalently Linked Protein Regulators02:04

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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.
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Spreading of Chromatin Modifications02:25

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The histone proteins in the nucleosomes are post-translationally modified (PTM) to increase or decrease access to DNA. The commonly observed PTMs are methylation, acetylation, phosphorylation, and ubiquitination of lysine amino acids in the histone H3 tail region. These histone modifications have specific meaning for the cell. Hence, they are called "histone code". The protein complex involved in histone modification is termed as "reader-writer" complex.
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Histone Modification02:32

Histone Modification

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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
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Phase II Reactions: Acetylation Reactions01:24

Phase II Reactions: Acetylation Reactions

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Acetylation, a phase II biotransformation reaction, introduces an acetyl group to drugs or their metabolites. Acetyltransferase enzymes facilitate this reaction, which resembles α-amino acid conjugation due to the addition of a functional group to the drug molecule.
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Mutagenicity and Carcinogenicity01:25

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Mutagenicity and carcinogenicity refer to the ability of drugs to cause genetic defects and induce cancer, respectively. The International Agency for Research on Cancer (IARC) classifies agents into four groups based on their carcinogenic potential. Group 1 agents are known human carcinogens; group 2A agents are probably carcinogenic to humans; group 3 agents lack data to support their role in carcinogenesis; and group 4 includes agents for which data support that they are not likely to be...
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Toxicological Assays for Testing Effects of an Epigenetic Drug on Development, Fecundity and Survivorship of Malaria Mosquitoes
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Acetylation-Mediated Epigenetic Consequences for Biological Control and Cancer.

Andrew J Fritz1,2,3, Kyle T McKay2,3,4, Haley W Greenyer1,2,3

  • 1Department of Biochemistry, University of Vermont, Burlington, VT, USA.

Results and Problems in Cell Differentiation
|July 1, 2025
PubMed
Summary

Histone acetylation epigenetically controls gene activity. Targeting this process offers new cancer treatment options by correcting abnormal gene expression and reducing side effects.

Keywords:
AcetylationEpigenetic controlHigher-order chromatin organizationPost-translational histone modificationsTranscription

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Area of Science:

  • Molecular Biology
  • Epigenetics
  • Cancer Biology

Background:

  • Histone acetylation epigenetically regulates gene transcription, influencing gene activation and suppression.
  • Acetylated histone states are crucial for gene promoter and enhancer activity, impacting regulatory protein interactions and chromatin organization.
  • Alterations in histone acetylation are linked to cell transformation and tumor progression.

Purpose of the Study:

  • To explore the role of histone acetylation in gene regulation and cancer.
  • To investigate the potential of targeting histone acetylation machinery for cancer therapy.

Main Methods:

  • Review of epigenetic mechanisms.
  • Analysis of histone acetylation's role in gene expression.
  • Exploration of therapeutic strategies targeting histone acetylation.

Main Results:

  • Histone acetylation dynamically controls gene transcription in response to physiological signals.
  • Acetylated histone states dictate gene promoter and enhancer activity, influencing chromatin structure.
  • Targeting histone acetylation machinery presents a promising avenue for cancer treatment, offering specificity and potentially fewer side effects.

Conclusions:

  • Histone acetylation is a key epigenetic regulator of gene expression.
  • Dysregulation of histone acetylation is implicated in cancer development.
  • Targeting histone acetylation pathways holds therapeutic potential for cancer treatment.