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Pharmaceuticals
Special Issues
Epigenetics as a Therapeutic Target in Human Diseases
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Epigenetics as a Therapeutic Target in Human Diseases

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

Deadline for manuscript submissions: closed (27 June 2023) | Viewed by 16577

Special Issue Editors

Dr. Olaia Martínez-Iglesias

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Guest Editor
Department of Medical Epigenetics, EuroEspes Biomedical Research Center, La Coruna, Spain
Interests: epigenetics; neurodegeneration; histones; DNA methylation; cancer; nutraceuticals
Dr. Iván Carrera

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Guest Editor
Department of Health Biotechnology, EuroEspes Biomedical Research Center, La Coruna, Spain
Interests: epigenetics; neurodegeneration; cancer; cerebrovascular diseases; nutraceuticals
Dr. Vinogran Naidoo

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Guest Editor
Department of Neurosciences, EuroEspes Biomedical Research Center, La Coruna, Spain
Interests: neurodegeneration; epigenetics; cancer; inflammation; pharmacology

Special Issue Information

Dear Colleagues,

Epigenetics is the study of heritable changes in gene expression that occur without alterations in the DNA sequence. The accumulation of epigenetic alterations over the lifespan may contribute to multifactorial diseases. Epigenetics is a broad area of research that is important for understanding basic cellular processes and the development of diseases. For the past few years, epigenetics has been advancing at a significant pace, creating great expectations in biology and medicine. Targeting the epigenetic apparatus with epigenetic drugs may be a promising strategy in the treatment of different diseases, including cancer, neurodegenerative disorders, and diabetes. Several epidrugs have already been approved for clinical use, including DNA methyltransferase (DNMT) and histone deacetylase (HDAC) inhibitors, such as azacitidine, vorinostat, romidepsin, and romidepsin. A considerable number of epigenetic compounds are presently being studied for the treatment of cancer, cardiovascular, immune, and central and peripheral nervous system pathologies, among others.

Unfortunately, the molecular processes underpinning the control of the epigenetic machinery are poorly understood, and the majority of available knowledge is fragmented. This limited understanding of epigenetic processes is a significant barrier in establishing the foundations of pharmacoepigenetics. Furthermore, there have been few studies on the pharmacogenetics and pharmacoepigenetics of contemporary drugs for the treatment of prevalent illnesses. This Special Issue on “Epigenetics as a Therapeutic Target in Human Diseases” aims to consolidate high-quality articles in the cutting-edge field of pharmacoepigenetics. Based on your leadership and expertise in this discipline, it would be an honor for us to be able to count on your collaboration in this Special Issue through the submission of a research article or review on epidrugs in human diseases.

Dr. Olaia Martínez-Iglesias
Dr. Iván Carrera
Dr. Vinogran Naidoo
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. 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
  • epidrug
  • DNA methylation
  • HDAC miRNAs
  • human diseases

Published Papers (7 papers)

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Review

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16 pages, 3269 KiB  
Review
Natural Products Treat Colorectal Cancer by Regulating miRNA
by Shuoxi Guo, Meiqi Chen, Shuangyang Li, Zijun Geng, Ye Jin and Da Liu
Pharmaceuticals 2023, 16(8), 1122; https://doi.org/10.3390/ph16081122 - 09 Aug 2023
Cited by 1 | Viewed by 1662
Abstract
Diseases are evolving as living standards continue to improve. Cancer is the main cause of death and a major public health problem that seriously threatens human life. Colorectal cancer is one of the top ten most common malignant tumors in China, ranking second [...] Read more.
Diseases are evolving as living standards continue to improve. Cancer is the main cause of death and a major public health problem that seriously threatens human life. Colorectal cancer is one of the top ten most common malignant tumors in China, ranking second after gastric cancer among gastrointestinal malignant tumors, and its incidence rate is increasing dramatically each year due to changes in the dietary habits and lifestyle of the world’s population. Although conventional therapies, such as surgery, chemotherapy, and radiotherapy, have profoundly impacted the treatment of colorectal cancer (CRC), drug resistance and toxicity remain substantial challenges. Natural products, such as dietary therapeutic agents, are considered the safest alternative for treating CRC. In addition, there is substantial evidence that natural products can induce apoptosis, inhibit cell cycle arrest, and reduce the invasion and migration of colon cancer cells by targeting and regulating the expression and function of miRNAs. Here, we summarize the recent research findings on the miRNA-regulation-based antitumor mechanisms of various active ingredients in natural products, highlighting how natural products target miRNA regulation in colon cancer prevention and treatment. The application of natural drug delivery systems and predictive disease biomarkers in cancer prevention and treatment is also discussed. Such approaches will contribute to the discovery of new regulatory mechanisms associated with disease pathways and provide a new theoretical basis for developing novel colon cancer drugs and compounds and identifying new therapeutic targets. Full article
(This article belongs to the Special Issue Epigenetics as a Therapeutic Target in Human Diseases)
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21 pages, 1691 KiB  
Review
Histone Modification of Colorectal Cancer by Natural Products
by Zijun Geng, Meiqi Chen, Qixuan Yu, Shuoxi Guo, Tianli Chen and Da Liu
Pharmaceuticals 2023, 16(8), 1095; https://doi.org/10.3390/ph16081095 - 02 Aug 2023
Cited by 1 | Viewed by 1783
Abstract
Natural products play important roles in the pathogenesis of many human malignancies, including colorectal cancer, and can act as a gene regulator in many cancers. They regulate malignant cell growth through many cellular signal pathways, including Rac family small GTPase 1 (RAC1)/PI3K/AKT (α-serine/threonine-protein [...] Read more.
Natural products play important roles in the pathogenesis of many human malignancies, including colorectal cancer, and can act as a gene regulator in many cancers. They regulate malignant cell growth through many cellular signal pathways, including Rac family small GTPase 1 (RAC1)/PI3K/AKT (α-serine/threonine-protein kinase), mitogen-activated protein kinase (MAPK), Wnt/β-catenin pathway, transforming growth factor-β (TGF-β), Janus kinase and signal transducer and activator of transcription (JAK-STAT), nuclear factor kappa-B (NF-κB), the Notch pathway, Hippo pathway, and Hedgehog pathway. In this review, we describe the epigenetic roles of several natural products, e.g., platycodin D (PD), ginsenoside Rd, tretinoin, Rutin, curcumin, clove extract, betulinic acid, resveratrol, and curcumin, in colorectal cancer, including their impact on colorectal cancer cell proliferation, apoptosis, invasion, migration, and anti-chemotherapeutic resistance. The aim is to illustrate the epigenetic mechanisms of action of natural products in cancer prevention and treatment, and to provide (1) a theoretical basis for the study of the role of epigenetics in influencing colorectal cancer; (2) new directions for studying the occurrence, development, and prognosis of colorectal cancer; and (3) new targets for treating and preventing colorectal cancer. Full article
(This article belongs to the Special Issue Epigenetics as a Therapeutic Target in Human Diseases)
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12 pages, 2856 KiB  
Review
Epigenetic Targets and Their Inhibitors in Thyroid Cancer Treatment
by Ke Zhang, Junyao Wang, Ziyan He, Xian Qiu, Ri Sa and Libo Chen
Pharmaceuticals 2023, 16(4), 559; https://doi.org/10.3390/ph16040559 - 07 Apr 2023
Cited by 1 | Viewed by 1916
Abstract
Although biologically targeted therapies based on key oncogenic mutations have made significant progress in the treatment of locally advanced or metastatic thyroid cancer, the challenges of drug resistance are urging us to explore other potentially effective targets. Herein, epigenetic modifications in thyroid cancer, [...] Read more.
Although biologically targeted therapies based on key oncogenic mutations have made significant progress in the treatment of locally advanced or metastatic thyroid cancer, the challenges of drug resistance are urging us to explore other potentially effective targets. Herein, epigenetic modifications in thyroid cancer, including DNA methylation, histone modifications, non-coding RNAs, chromatin remodeling and RNA alterations, are reviewed and epigenetic therapeutic agents for the treatment of thyroid cancer, such as DNMT (DNA methyltransferase) inhibitors, HDAC (histone deacetylase) inhibitors, BRD4 (bromodomain-containing protein 4) inhibitors, KDM1A (lysine demethylase 1A) inhibitors and EZH2 (enhancer of zeste homolog 2) inhibitors, are updated. We conclude that epigenetics is promising as a therapeutic target in thyroid cancer and further clinical trials are warranted. Full article
(This article belongs to the Special Issue Epigenetics as a Therapeutic Target in Human Diseases)
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24 pages, 2050 KiB  
Review
Natural Bioactive Products as Epigenetic Modulators for Treating Neurodegenerative Disorders
by Olaia Martínez-Iglesias, Vinogran Naidoo, Iván Carrera, Lola Corzo and Ramón Cacabelos
Pharmaceuticals 2023, 16(2), 216; https://doi.org/10.3390/ph16020216 - 31 Jan 2023
Cited by 5 | Viewed by 2355
Abstract
Neurodegenerative disorders (NDDs) are major health issues in Western countries. Despite significant efforts, no effective therapeutics for NDDs exist. Several drugs that target epigenetic mechanisms (epidrugs) have been recently developed for the treatment of NDDs, and several of these are currently being tested [...] Read more.
Neurodegenerative disorders (NDDs) are major health issues in Western countries. Despite significant efforts, no effective therapeutics for NDDs exist. Several drugs that target epigenetic mechanisms (epidrugs) have been recently developed for the treatment of NDDs, and several of these are currently being tested in clinical trials. Furthermore, various bioproducts have shown important biological effects for the potential prevention and treatment of these disorders. Here, we review the use of natural products as epidrugs to treat NDDs in order to explore the epigenetic effects and benefits of functional foods and natural bioproducts on neurodegeneration. Full article
(This article belongs to the Special Issue Epigenetics as a Therapeutic Target in Human Diseases)
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27 pages, 2527 KiB  
Review
Epigenetics as a Therapeutic Target in Osteoarthritis
by Carmen Núñez-Carro, Margarita Blanco-Blanco, Karla Mariuxi Villagrán-Andrade, Francisco J. Blanco and María C. de Andrés
Pharmaceuticals 2023, 16(2), 156; https://doi.org/10.3390/ph16020156 - 21 Jan 2023
Cited by 5 | Viewed by 2426
Abstract
Osteoarthritis (OA) is a heterogenous, complex disease affecting the integrity of diarthrodial joints that, despite its high prevalence worldwide, lacks effective treatment. In recent years it has been discovered that epigenetics may play an important role in OA. Our objective is to review [...] Read more.
Osteoarthritis (OA) is a heterogenous, complex disease affecting the integrity of diarthrodial joints that, despite its high prevalence worldwide, lacks effective treatment. In recent years it has been discovered that epigenetics may play an important role in OA. Our objective is to review the current knowledge of the three classical epigenetic mechanisms—DNA methylation, histone post-translational modifications (PTMs), and non-coding RNA (ncRNA) modifications, including microRNAs (miRNAs), circular RNAs (circRNAs), and long non-coding RNAs (lncRNAs)—in relation to the pathogenesis of OA and focusing on articular cartilage. The search for updated literature was carried out in the PubMed database. Evidence shows that dysregulation of numerous essential cartilage molecules is caused by aberrant epigenetic regulatory mechanisms, and it contributes to the development and progression of OA. This offers the opportunity to consider new candidates as therapeutic targets with the potential to attenuate OA or to be used as novel biomarkers of the disease. Full article
(This article belongs to the Special Issue Epigenetics as a Therapeutic Target in Human Diseases)
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20 pages, 1267 KiB  
Review
Epigenetic Regulation of Macrophage Polarization in Cardiovascular Diseases
by Sumra Komal, Sheng-Na Han, Liu-Gen Cui, Miao-Miao Zhai, Yue-Jiao Zhou, Pei Wang, Muhammad Shakeel and Li-Rong Zhang
Pharmaceuticals 2023, 16(2), 141; https://doi.org/10.3390/ph16020141 - 18 Jan 2023
Cited by 6 | Viewed by 3467
Abstract
Cardiovascular diseases (CVDs) are the leading cause of hospitalization and death worldwide, especially in developing countries. The increased prevalence rate and mortality due to CVDs, despite the development of several approaches for prevention and treatment, are alarming trends in global health. Chronic inflammation [...] Read more.
Cardiovascular diseases (CVDs) are the leading cause of hospitalization and death worldwide, especially in developing countries. The increased prevalence rate and mortality due to CVDs, despite the development of several approaches for prevention and treatment, are alarming trends in global health. Chronic inflammation and macrophage infiltration are key regulators of the initiation and progression of CVDs. Recent data suggest that epigenetic modifications, such as DNA methylation, posttranslational histone modifications, and RNA modifications, regulate cell development, DNA damage repair, apoptosis, immunity, calcium signaling, and aging in cardiomyocytes; and are involved in macrophage polarization and contribute significantly to cardiac disease development. Cardiac macrophages not only trigger damaging inflammatory responses during atherosclerotic plaque formation, myocardial injury, and heart failure but are also involved in tissue repair, remodeling, and regeneration. In this review, we summarize the key epigenetic modifications that influence macrophage polarization and contribute to the pathophysiology of CVDs, and highlight their potential for the development of advanced epigenetic therapies. Full article
(This article belongs to the Special Issue Epigenetics as a Therapeutic Target in Human Diseases)
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Other

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9 pages, 933 KiB  
Brief Report
Up-Regulation of PSMA Expression In Vitro as Potential Application in Prostate Cancer Therapy
by Roswitha Runge, Anne Naumann, Matthias Miederer, Joerg Kotzerke and Claudia Brogsitter
Pharmaceuticals 2023, 16(4), 538; https://doi.org/10.3390/ph16040538 - 04 Apr 2023
Cited by 1 | Viewed by 1738
Abstract
Possibilities to improve the therapeutic efficacy of Lu-177–PSMA-617 radionuclide therapy by modulation of target expression are being investigated. Knowledge on regulatory factors that promote prostate cancer (PCa) progression may contribute to targeting prostate cancer more effectively. We aimed at the stimulation of PCa [...] Read more.
Possibilities to improve the therapeutic efficacy of Lu-177–PSMA-617 radionuclide therapy by modulation of target expression are being investigated. Knowledge on regulatory factors that promote prostate cancer (PCa) progression may contribute to targeting prostate cancer more effectively. We aimed at the stimulation of PCa cell lines using the substances 5-aza-2′-deoxycitidine (5-aza-dC) and valproic acid (VPA) to achieve increased prostate-specific membrane antigen (PSMA) expression. PC3, PC3-PSMA, and LNCaP cells were incubated with varying concentrations of 5-aza-dC and VPA to investigate the cell-bound activity of Lu-177–PSMA-617. Stimulation effects on both the genetically modified cell line PC3-PSMA and the endogenously PSMA-expressing LNCaP cells were demonstrated by increased cellular uptake of the radioligand. For PC3-PSMA cells, the fraction of cell-bound radioactivity was enhanced by about 20-fold compared to that of the unstimulated cells. Our study reveals an increased radioligand uptake mediated by stimulation for both PC3-PSMA and LNCaP cell lines. In perspective of an enhanced PSMA expression, the present study might contribute to advanced radionuclide therapy approaches that improve the therapeutic efficacy, as well as combined treatment options. Full article
(This article belongs to the Special Issue Epigenetics as a Therapeutic Target in Human Diseases)
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