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Molecules
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Next Generation Histone Deacetylase (HDAC) Inhibitors
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Next Generation Histone Deacetylase (HDAC) Inhibitors

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Chemical Biology".

Deadline for manuscript submissions: closed (31 January 2019) | Viewed by 8913

Special Issue Editors

Prof. Dr. Thomas Kurz

E-Mail Website
Guest Editor
Heinrich-Heine-Universität Düsseldorf, Institute for Pharmaceutical and Medicinal Chemistry, Universitätsstraße 1, 40225 Düsseldorf, Germany
Interests: anti-infective drug discovery; epigenetic drug discovery; metalloenzyme inhibitors; protein-protein interactions; multi-target drugs
Prof. Dr. Finn K. Hansen

E-Mail Website
Guest Editor
Institute of Pharmacy, Leipzig University, Brüderstraße 34, 04103 Leipzig, Germany
Interests: HDAC inhibitors; epigenetics; multi-target drugs; foldamers; peptidomimetics

Special Issue Information

Dear Colleagues,

Histone deacetylases (HDACs) are clinically validated epigenetic drug targets for the treatment of cancer. Thus far, four histone deacetylase inhibitors (HDACi) have been approved by the FDA to combat certain types of lymphoma or multiple myeloma. Furthermore, there is growing evidence that HDACi have therapeutic potential in several diseases beyond cancer, such as inflammation, HIV, and parasitic and neurodegenerative diseases. First-generation inhibitors are non-selective HDACi that target multiple isoforms which might lead to serious side effect. In the field of cancer, it is currently under debate whether class- or isoform-selective HDACi can provide improved risk-benefit profiles compared to first-generation pan-inhibitors. In the field of non-oncology diseases, it is evident that the use of pan-HDACi is limited due to their side effects. Thus, there is a strong need for new HDACi with optimized selectivity profiles.

The aim of this Special Issue is to highlight recent efforts in the design, synthesis, and pharmacological evaluation of next-generation histone deacetylase inhibitors. We welcome original articles and short communications as well as review articles.

Prof. Dr. Thomas Kurz
Prof. Dr. Finn K. Hansen
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • HDAC inhibitors
  • epigenetics
  • drug design
  • chromatin modification
  • chemical probe and assay development

Published Papers (2 papers)

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Review

18 pages, 712 KiB  
Review
Regulation of Osteoclast Differentiation and Skeletal Maintenance by Histone Deacetylases
by Bora Faulkner, Kristina Astleford and Kim C. Mansky
Molecules 2019, 24(7), 1355; https://doi.org/10.3390/molecules24071355 - 06 Apr 2019
Cited by 25 | Viewed by 4764
Abstract
Bone is a dynamic tissue that must respond to developmental, repair, and remodeling cues in a rapid manner with changes in gene expression. Carefully-coordinated cycles of bone resorption and formation are essential for healthy skeletal growth and maintenance. Osteoclasts are large, multinucleated cells [...] Read more.
Bone is a dynamic tissue that must respond to developmental, repair, and remodeling cues in a rapid manner with changes in gene expression. Carefully-coordinated cycles of bone resorption and formation are essential for healthy skeletal growth and maintenance. Osteoclasts are large, multinucleated cells that are responsible for breaking down bone by secreting acids to dissolve the bone mineral and proteolytic enzymes that degrade the bone extracellular matrix. Increased osteoclast activity has a severe impact on skeletal health, and therefore, osteoclasts represent an important therapeutic target in skeletal diseases, such as osteoporosis. Progression from multipotent progenitors into specialized, terminally-differentiated cells involves carefully-regulated patterns of gene expression to control lineage specification and emergence of the cellular phenotype. This process requires coordinated action of transcription factors with co-activators and co-repressors to bring about proper activation and inhibition of gene expression. Histone deacetylases (HDACs) are an important group of transcriptional co-repressors best known for reducing gene expression via removal of acetyl modifications from histones at HDAC target genes. This review will cover the progress that has been made recently to understand the role of HDACs and their targets in regulating osteoclast differentiation and activity and, thus, serve as potential therapeutic target. Full article
(This article belongs to the Special Issue Next Generation Histone Deacetylase (HDAC) Inhibitors)
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15 pages, 449 KiB  
Review
Role of Natural Products in Modulating Histone Deacetylases in Cancer
by Myriam Merarchi, Gautam Sethi, Muthu K. Shanmugam, Lu Fan, Frank Arfuso and Kwang Seok Ahn
Molecules 2019, 24(6), 1047; https://doi.org/10.3390/molecules24061047 - 16 Mar 2019
Cited by 48 | Viewed by 3850
Abstract
Histone deacetylases (HDACs) are enzymes that can control transcription by modifying chromatin conformation, molecular interactions between the DNA and the proteins as well as the histone tail, through the catalysis of the acetyl functional sites removal of proteins from the lysine residues. Also, [...] Read more.
Histone deacetylases (HDACs) are enzymes that can control transcription by modifying chromatin conformation, molecular interactions between the DNA and the proteins as well as the histone tail, through the catalysis of the acetyl functional sites removal of proteins from the lysine residues. Also, HDACs have been implicated in the post transcriptional process through the regulation of the proteins acetylation, and it has been found that HDAC inhibitors (HDACi) constitute a promising class of pharmacological drugs to treat various chronic diseases, including cancer. Indeed, it has been demonstrated that in several cancers, elevated HDAC enzyme activities may be associated with aberrant proliferation, survival and metastasis. Hence, the discovery and development of novel HDACi from natural products, which are known to affect the activation of various oncogenic molecules, has attracted significant attention over the last decade. This review will briefly emphasize the potential of natural products in modifying HDAC activity and thereby attenuating initiation, progression and promotion of tumors. Full article
(This article belongs to the Special Issue Next Generation Histone Deacetylase (HDAC) Inhibitors)
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