Histone Deacetylase Inhibitors and Anaplastic Thyroid Carcinoma

Eleftherios Spartalis1, Dimitrios I Athanasiadis2, Dimosthenis Chrysikos3

  • 1Laboratory of Experimental Surgery and Surgical Research N.S. Christeas, Medical School, National and Kapodistrian University of Athens, Athens, Greece eleftherios.spartalis@gmail.com.

Anticancer Research
|March 8, 2019
PubMed
Abstract

Insights

Histone deacetylase inhibitors (HDACI) show promise for treating anaplastic thyroid cancer (ATC), an aggressive malignancy. Research indicates HDACI are effective as standalone treatments or in combination therapies for ATC management.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Anaplastic thyroid cancer (ATC) is a highly aggressive and often incurable human malignancy.
  • Histone deacetylases (HDAC) are implicated in regulating gene transcription within ATC.
  • HDAC inhibitors (HDACI) are emerging as potential therapeutic agents for ATC.

Purpose of the Study:

  • To review the efficacy of HDAC inhibitors in treating anaplastic thyroid cancer.
  • To outline current research trends concerning HDACIs in ATC.

Main Methods:

  • A literature review was conducted using the MEDLINE database.
  • Search terms included "thyroid cancer," "anaplastic," "HDAC," "histone," "deacetylase*," and "HDACI."

Main Results:

  • Numerous compounds, including valproic acid, trichostatin A, panobinostat, belinostat, and others, demonstrated significant antitumor activity against ATC.
  • Specific compounds like SuberoylAnilide Hydroxamic Acid, AB1-13, MS-275, depsipeptide, CUDC101, CUDC907, HNHA, and PXD101 were highlighted for their effects.

Conclusions:

  • HDAC inhibitors represent a promising therapeutic strategy for managing anaplastic thyroid cancer.
  • HDACIs show potential efficacy when used as monotherapy or in combination with other anticancer agents.

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...
16.1K
Histone Modification02:32

Histone Modification

4.5K
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...
11.0K
Histone Variants at the Centromere02:30

Histone Variants at the Centromere

Histone variants are the histone proteins with structural and sequence variations. These variants may be regarded as “mutant” forms that replace their canonical histone counterparts in the nucleosomes. Specific post-translational modifications on the histone variants enable further chromatin complexity and regulate tissue-specific gene expression. The most common histone variants are from histone H2A, H2B, and linker histone H1 families. However, several variants of histone H3...
5.0K
Co-activators and Co-repressors02:04

Co-activators and Co-repressors

Gene transcription is regulated by the synergistic action of several proteins that form a complex at a gene regulatory site. This is observed in eukaryotes, where the regulation of gene expression is a complex process. Regulatory proteins in eukaryotes can broadly be classified into two types – regulators that bind directly to specific DNA sequences and co-regulators that associate with regulatory proteins but cannot directly bind to the DNA. These co-regulators are further divided into...
8.6K
The Thyroid Gland01:23

The Thyroid Gland

The thyroid gland is a small, butterfly-shaped gland located in the neck and covers the anterior surface of the trachea. The gland has two lateral lobes connected by a thin tissue mass called the isthmus. Internally, each lobe comprises many small spherical structures known as thyroid follicles, surrounded by a network of blood vessels.
The follicles have a central cavity lined by simple cuboidal to squamous epithelial cells called follicular cells. These cells produce the glycoprotein...
7.6K