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Pharmaceuticals
Special Issues
New Therapeutic Opportunities for Epigenetic Drugs
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New Therapeutic Opportunities for Epigenetic Drugs

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Biopharmaceuticals".

Deadline for manuscript submissions: closed (20 November 2024) | Viewed by 4789

Special Issue Editor

Dr. Sebastiano Giallongo

E-Mail Website
Guest Editor
Department of Biomedical Sciences (BIOMED), Surgical Sciences and Advanced Technologies “G.F. Ingrassia”, University of Catania, Catania, Italy
Interests: epigenetics; metabolism; aging; hematological malignancies; tumor microenvironment
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Recent advancements have highlighted the potential of targeting epigenetic regulators, using epigenetic drugs, to treat a variety of diseases, leveraging the ability to modulate gene expression without altering the DNA sequence. This approach offers precision in tackling conditions such as cancer, neurological disorders, and autoimmune diseases. Generally, the usage of these drugs may represent a novel advancement towards personalized medicine. Innovative methodologies, including CRISPR-based epigenome editing, small molecule inhibitors, and protein-based therapeutics, are showing promising results in both preclinical and clinical trials. For instance, small molecule inhibitors targeting histone deacetylases (HDACs) and DNA methyltransferases (DNMTs) have demonstrated significant efficacy in reactivating silenced genes and altering disease pathways. Additionally, the specificity and reversibility of these therapies provide a compelling advantage, paving the way for a more effective treatment strategy. The potential for these epigenetic therapies to be combined with existing treatments also offers a synergistic approach, potentially enhancing therapeutic outcomes and reducing adverse effects.

This Special Issue aims to summarize the state of the art about the current advances in targeting epigenetic regulators, such as CRISPR-based editing and small molecule inhibitors. These show promise in treating cancer, neurological disorders, and autoimmune diseases, thus modulating gene expression without altering DNA and providing a compelling advantage for personalized medicine and more effective treatments.

Dr. Sebastiano Giallongo
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. Pharmaceuticals 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 2900 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

  • epigenetics
  • aging
  • personalized medicine
  • tumor microenvironment
  • DNA methyltransferase
  • histone acetyltransferase
  • histone deacetylases
  • histone variants
  • epigenetics-metabolism axis

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Published Papers (2 papers)

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22 pages, 4847 KiB  
Article
Increased MAGE-C Family Gene Expression Levels as a Biomarker of Colon Cancer Through the Demethylation Mechanism
by Mikhlid H. Almutairi, Waad A. Alsoraie, Turki M. Alrubie, Ahmad S. Alkhaldi, Nada S. Alhajri, Monira A. Alaujan, Manar H. Almutairi and Bader O. Almutairi
Pharmaceuticals 2024, 17(11), 1447; https://doi.org/10.3390/ph17111447 - 29 Oct 2024
Viewed by 1434
Abstract
Background/Objectives: Colon cancer (CC) in Saudi Arabia is associated with a high death rate and is commonly identified at a more progressive stage. Therefore, it is critical to identify and characterize potential novel cancer-specific biomarkers to enhance early CC diagnosis. The goal was [...] Read more.
Background/Objectives: Colon cancer (CC) in Saudi Arabia is associated with a high death rate and is commonly identified at a more progressive stage. Therefore, it is critical to identify and characterize potential novel cancer-specific biomarkers to enhance early CC diagnosis. The goal was to assess their potential use as cancer biomarkers for the early detection and improvement of CC treatment. Methods: MAGE-C1, MAGE-C2, and MAGE-C3 family gene expression levels were examined using RT-PCR and qRT-PCR assays in 26 adjacent normal colon (NC) and CC tissue samples from male and female Saudi patients. Using several cell lines and the qRT-PCR technique, epigenetic control was also investigated to determine whether reduced treatment with 5-aza-2′-deoxycytidine, which reduces DNA methyltransferase, can increase the expression of the MAGE-C gene. The expression levels, promoter methylation, and prognostic significance of MAGE-C1, MAGE-C2, and MAGE-C3 genes across various cancers were analyzed using The Cancer Genome Atlas (TCGA) data. Additionally, the prognostic significance of these genes was assessed through Kaplan–Meier survival analysis. Results: The RT-PCR results showed that MAGE-C1, MAGE-C2, and MAGE-C3 gene expressions were significantly higher in the CC and NC tissues. The MAGE-C1 expression level was the highest in CC tissues (p < 0.0001), followed by MAGE-C3 (p = 0.0004) and MAGE-C2 (p = 0.0020) in descending order. The 5-aza-2′-deoxycytidine treatment significantly increased the mRNA expression levels of the MAGE-C1, MAGE-C2, and MAGE-C3 genes in HCT116, Caco-2, MCF-7, and MCF-10A cells. Expression analyses of TCGA samples revealed significant upregulation of these genes in several cancer types, with notable differences between normal, tumor, and metastatic tissues. Promoter methylation indicates hypomethylation in cancerous tissues. Survival analyses show that high expression levels of MAGE-C1 correlate with better prognosis, while MAGE-C3 is associated with poorer outcomes. Conclusions: These results demonstrate that MAGE-C genes are viable prospective biomarkers of CC controlled by hypomethylating drugs, consequently offering a possible treatment target for CC in a specific population. Full article
(This article belongs to the Special Issue New Therapeutic Opportunities for Epigenetic Drugs)
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15 pages, 1895 KiB  
Article
Fish Oil Containing Pro-Resolving Mediators Enhances the Antioxidant System and Ameliorates LPS-Induced Inflammation in Human Bronchial Epithelial Cells
by Alfio Distefano, Laura Orlando, Sebastiano Giallongo, Emanuela Tropea, Mariarita Spampinato, Annalisa Santisi, Lucia Longhitano, Giuseppe Parisi, Salvatore Leonardi, Arcangelo Russo, Massimo Caruso, Michelino Di Rosa, Daniele Tibullo, Maurizio Salamone, Giovanni Li Volti and Ignazio Alberto Barbagallo
Pharmaceuticals 2024, 17(8), 1066; https://doi.org/10.3390/ph17081066 - 14 Aug 2024
Viewed by 3007
Abstract
Fish oil, renowned for its high content of omega-3 fatty acids, particularly eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), has gained considerable attention for its potential health benefits. EPA and DHA exhibit anti-inflammatory effects by promoting the production of specialized pro-resolving mediators (SPMs), [...] Read more.
Fish oil, renowned for its high content of omega-3 fatty acids, particularly eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), has gained considerable attention for its potential health benefits. EPA and DHA exhibit anti-inflammatory effects by promoting the production of specialized pro-resolving mediators (SPMs), such as resolvins and protectins. Fish oil has been studied for its potential to reduce bronchial inflammation, a key feature of respiratory conditions like asthma and COPD. This study investigates the cellular mechanisms of fish oil in an in vitro model of lung inflammation using lipopolysaccharide (LPS) on a healthy human bronchial epithelium cell line. LPS exposure for 24 h reduced cell viability, elevated reactive oxygen species (ROS), depleted glutathione (GSH), and induced mitochondrial depolarization, indicating oxidative stress and inflammation. Fish oil administration significantly mitigated ROS production, prevented GSH depletion, and reduced mitochondrial depolarization. This was associated with the upregulation of the endogenous antioxidant system, evidenced by restored GSH levels and the increased gene expression of glutathione peroxidase (GPX), catalase (CAT), superoxide dismutase 1 (SOD1), and superoxide dismutase 2 (SOD2). Fish oil also suppressed IL-6 and IL-1β expression and increased anti-inflammatory cytokine IL-10 expression. Furthermore, fish oil upregulated the expression of pro-resolving mediator receptors, suggesting a role in inflammation resolution. These findings highlight the potential of fish oil supplementation as a preventive measure against pulmonary diseases characterized by unresolved inflammation such as lung inflammation. Full article
(This article belongs to the Special Issue New Therapeutic Opportunities for Epigenetic Drugs)
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