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Related Concept Videos

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,...
Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a DNA...
Heterochromatin02:38

Heterochromatin

The extent of chromatin compaction can be studied by staining chromatin using specific DNA binding dyes. Under the microscope, the dense-compacted regions that take up more dye are called heterochromatin. Heterochromatin is further classified into two forms – constitutive heterochromatin and facultative heterochromatin.
Constitutive heterochromatin: It is a highly compact region of chromatin that is mostly concentrated in the centromere and telomere. Unlike euchromatin, the amino acid at 9th...
Chromatin Modification in iPS Cells01:32

Chromatin Modification in iPS Cells

Chromatin modification alters gene expression; therefore, scientists can add histone-modifying enzymes, histone variants, and chromatin remodeling complexes to somatic cells to aid reprogramming into pluripotent stem (iPS) cells.
Compact chromatin makes reprogramming difficult. Enzymes, such as histone demethylases and acetyltransferases, are often added during reprogramming to loosen the chromatin, making the DNA more accessible to transcription factors. Molecules that inhibit histone...
Antiviral Nucleoside Inhibitors01:22

Antiviral Nucleoside Inhibitors

Antiviral Nucleoside InhibitorsAntiviral nucleoside inhibitors are structural analogs of natural nucleosides that interfere with viral DNA or RNA synthesis. These compounds selectively target viral polymerases due to their resemblance to host nucleosides, thereby disrupting viral genome replication.Mechanism of Acyclovir ActionAcyclovir is a guanosine analog with a three-carbon acyclic side chain. It selectively targets herpes simplex virus type 1 (HSV-1), herpes simplex virus type 2 (HSV-2),...

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Updated: Jul 4, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

Isoform-selective histone deacetylase inhibitors.

Anton V Bieliauskas1, Mary Kay H Pflum

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

Chemical Society Reviews
|June 24, 2008
PubMed
Summary

Developing selective histone deacetylase (HDAC) inhibitors is crucial for cancer therapy. This review highlights progress in creating HDAC inhibitors that target specific HDAC classes and isoforms, exploiting active site differences for better drug design.

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Assays for Validating Histone Acetyltransferase Inhibitors
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Examination of Proteins Bound to Nascent DNA in Mammalian Cells Using BrdU-ChIP-Slot-Western Technique

Published on: January 14, 2016

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Histone deacetylase (HDAC) proteins are key regulators of gene transcription and are implicated in various cancers.
  • Numerous small molecule HDAC inhibitors are under investigation as anti-cancer therapeutics, with many in clinical trials.
  • Current HDAC inhibitors often lack selectivity, affecting multiple HDAC isoforms across different classes.

Purpose of the Study:

  • To review recent advancements in the development of class-selective and isoform-selective HDAC inhibitors.
  • To explore strategies for achieving selectivity based on structural differences in HDAC active sites.
  • To provide insights into emerging trends in targeted HDAC inhibition for cancer treatment.

Main Methods:

  • Literature review of recent research on HDAC inhibitor development.
  • Analysis of studies focusing on structure-activity relationships for HDAC isoform selectivity.
  • Discussion of emerging trends and future directions in targeted HDAC inhibition.

Main Results:

  • Significant progress has been made in identifying HDAC inhibitors with improved class and isoform selectivity.
  • Subtle differences within the active sites of HDAC isoforms present opportunities for designing targeted inhibitors.
  • Emerging trends indicate a shift towards precision medicine approaches in HDAC inhibitor development.

Conclusions:

  • Targeted inhibition of specific HDAC isoforms holds promise for more effective and less toxic cancer therapies.
  • Exploiting active site variations is a key strategy for achieving desired selectivity in HDAC inhibitor design.
  • Continued research in this area is essential for advancing the clinical application of HDAC inhibitors in oncology.