Histone Deacetylase and Its Inhibitors: Drug Discovery, Molecular Mechanism, and Clinical Implications

A special issue of Biomedicines (ISSN 2227-9059). This special issue belongs to the section "Drug Discovery, Development and Delivery".

Deadline for manuscript submissions: 30 April 2024 | Viewed by 468

Special Issue Editor


E-Mail Website
Guest Editor
National Research Council, Rome, Italy
Interests: schistosomiasis; biochemistry; HDACs inhibitors; crystallography; phylogenetics; drug discovery; drug repurposing
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

On behalf of the Biomedicines Editorial Board and policies, I am pleased to announce the upcoming Special Issue entitled Histone Deacetylase and its Inhibitors: Molecular Mechanism and Clinical Implications. Histone deacetylases (HDACs) emerged as leading characters in many physiopathological aspects of human health and disease, thus entering the list of peculiar targets for pharmaceutical interventions. HDACs are important modulators of several cellular activities in their main function of chromatin remodeling enzymes. Their role does not only rely on epigenetics control but it is also directed toward many cytosolic partner proteins. HDACs are also elective targets to cope with organisms of social and clinical relevance, such as Plasmodium (causing malaria) and Schistosomiasis. Thus, HDACs are the subject of many drug discovery campaigns whose main goal is to specifically target precise isoforms.

We foster the submission of experimental papers dealing with original findings in the field of medicinal chemistry and biochemistry, with particular emphasis devoted to drug discovery and drug repurposing. We encourage the submission of papers reporting functional and biomolecular data and molecular mechanisms of action of new inhibitors; papers reporting virtual screening approach followed by or based on a clear correlation with functional in vitro/in vivo data are also greatly encouraged to be submitted, as well as papers that try to deepen molecular mechanism and dynamics. Clinical-relevant papers that mainly propose the use of already known drugs are also welcome. The final goal of the Special Issue is to propose original papers dealing with the discovery and/or repurposing of drugs that may target HDAC in the most specific manner by providing experimental evidence of their binding site to the enzyme, their mechanism of action, and their potential therapeutic impact. So far, the vast majority of HDACs’ inhibitors act by chelating the catalytic metal in the active site(s) of the enzyme, irrespective of the isoform to whom it is directed. We aim to screen additional possibilities of inhibition, either mechanism-based or targeting at different binding sites.

Dr. Fulvio Saccoccia
Guest Editor

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. Biomedicines is an international peer-reviewed open access monthly 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 2600 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

  • HDACs inhibitors
  • molecular mechanism
  • molecular dynamics
  • virtual screening

Published Papers (1 paper)

Order results
Result details
Select all
Export citation of selected articles as:

Research

16 pages, 576 KiB  
Article
Clinical Significance of the Immunohistochemical Expression of Histone Deacetylases (HDACs)-2, -4, and -5 in Ovarian Adenocarcinomas
by Georgia Levidou, Dimitrios Arsenakis, Dimitrios I. Bolovis, Roxanne Meyer, Cosima V. M. Brucker, Thomas Papadopoulos and Stamatios Theocharis
Biomedicines 2024, 12(5), 947; https://doi.org/10.3390/biomedicines12050947 (registering DOI) - 24 Apr 2024
Viewed by 189
Abstract
Background: Histone deacetylases (HDACs) are implicated in carcinogenesis, and HDAC inhibitors (HDACis) are explored as a therapeutic tool in several tumors. The aim of this study was to evaluate the clinical significance of HDAC-2, -4, and -5 expression in epithelial ovarian carcinoma (EOC). [...] Read more.
Background: Histone deacetylases (HDACs) are implicated in carcinogenesis, and HDAC inhibitors (HDACis) are explored as a therapeutic tool in several tumors. The aim of this study was to evaluate the clinical significance of HDAC-2, -4, and -5 expression in epithelial ovarian carcinoma (EOC). Methods: HDAC-2, -4, and -5 immunohistochemical expression was examined in 92 EOC tissue specimens and was correlated with clinicopathological characteristics. Results: HDAC-2 was the most frequently (94.4%) expressed isoform, being marginally higher in serous tumors compared with other types (p = 0.08). HDAC-5 was the less frequently expressed (28.1%), being positively associated with HDAC-4. HDAC-4 positivity was associated with lower FIGO-stage (p = 0.045) and T-category (p = 0.043) and the absence of lymph node (p = 0.05) or distant metastasis (p = 0.09) in serous carcinomas. HDAC-2 positivity was correlated with the absence of lymph node metastasis in serous tumors (p = 0.045). On the contrary, HDAC-5 nuclear positivity was correlated with lymph node metastasis in the entire cohort (p = 0.048). HDAC-4 positivity was marginally associated with favorable prognosis in serous carcinomas in univariate survival analysis (p = 0.086), but this correlation was not significant in multivariate analysis. Conclusions: These findings suggest a differential expression among HDAC-2, -4, and -5 in ovarian adenocarcinomas in terms of immunolocalization, positivity rate, and associations with clinicopathological parameters, providing evidence for a potential role in the pathobiology of EOC. Full article
Back to TopTop