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Related Concept Videos

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),...
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
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Inhibitors of Viral Protein Synthesis01:30

Inhibitors of Viral Protein Synthesis

Protein synthesis is indispensable for viral replication, as viruses lack the cellular machinery required for this process and must hijack the host's translational apparatus. In response, host cells deploy a critical innate immune defense involving interferons, specialized cytokines that play a central role in inhibiting viral propagation.Upon viral detection, infected cells release interferons that bind to receptors on adjacent uninfected cells, activating the JAK-STAT signaling pathway and...
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...
Anaphase Promoting Complex00:50

Anaphase Promoting Complex

The stepwise destruction of specific proteins is necessary for the progression and completion of the cell cycle. Such proteins are ubiquitinated by ubiquitin ligases and then subsequently destroyed by the proteasome. The SCF (Skp1/Cullin/F-box) and the anaphase-promoting complex (APC) are two important ubiquitin ligases involved in cell cycle progression. While SCF is active throughout the cell cycle, APC gets activated during metaphase to anaphase transition. Cdc20 or Cdh1 binds to APC and...

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Updated: Jun 12, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

Macrocyclic histone deacetylase inhibitors.

Sandra C Mwakwari1, Vishal Patil, William Guerrant

  • 1Parker H. Petit Institute of Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, 30332-0400, USA.

Current Topics in Medicinal Chemistry
|June 12, 2010
PubMed
Summary

Histone deacetylase inhibitors (HDACi) are novel anti-cancer drugs. This review focuses on macrocyclic HDACi, highlighting their complex structures and potent, selective inhibition of HDAC enzymes for therapeutic applications.

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Purification of H3 and H4 Histone Proteins and the Quantification of Acetylated Histone Marks in Cells and Brain Tissue
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Purification of H3 and H4 Histone Proteins and the Quantification of Acetylated Histone Marks in Cells and Brain Tissue

Published on: November 30, 2018

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Oncology

Background:

  • Histone deacetylase inhibitors (HDACi) represent a promising therapeutic class with demonstrated anti-cancer effects.
  • HDACi also show potential in treating parasitic, neurodegenerative, rheumatologic, and autoimmune diseases.
  • Small molecule HDACi encompass diverse structures like aryl hydroxamates, benzamides, and macrocyclic peptides.

Purpose of the Study:

  • To review recent advancements in the field of macrocyclic HDAC inhibitors.
  • To discuss the current status and therapeutic potential of macrocyclic HDACi.

Main Methods:

  • Literature review of scientific publications on macrocyclic HDAC inhibitors.
  • Analysis of structural features and inhibitory activity of macrocyclic HDACi.
  • Evaluation of isoform selectivity and potency of macrocyclic HDACi.

Main Results:

  • Macrocyclic HDACi exhibit complex cap-group structures that interact with the HDAC enzyme's outer rim.
  • These compounds demonstrate potent HDAC inhibition and high isoform selectivity.
  • Recent progress indicates significant potential for macrocyclic HDACi in various therapeutic areas.

Conclusions:

  • Macrocyclic HDAC inhibitors are a significant area of research within HDACi development.
  • Their unique structural attributes contribute to potent and selective enzyme inhibition.
  • Further investigation into macrocyclic HDACi is warranted for their clinical application.