Review
Pharmacology & Pharmacy
Meran Keshawa Ediriweera
Summary: Histone acetylation is a crucial epigenetic event and continues to be an area of great interest in biochemical research. The balance between histone acetyltransferases (HATs) and histone deacetylases (HDACs) is disrupted in various human cancers. Histone deacetylase inhibitors (HDACi) have shown promising results in restoring dysregulated histone acetylation profiles and are considered as potential anti-cancer therapeutics. Recent studies have identified odd-chain fatty acids as novel HDACi, further expanding the understanding of fatty acids in cancer therapy.
DRUG DISCOVERY TODAY
(2023)
Review
Oncology
Md Sahab Uddin, Abdullah Al Mamun, Badrah S. Alghamdi, Devesh Tewari, Philippe Jeandet, Md Shahid Sarwar, Ghulam Md Ashraf
Summary: Research has shown that glioma progression is closely linked to different types of epigenetic phenomena, such as chromatin modifications, DNA methylation, chromatin remodeling, and aberrant microRNA. Targeting the genes and proteins that control these alterations can be an effective way to treat GBM. Treatment approaches include histone deacetylase inhibitors and DNA methyltransferase inhibitors.
SEMINARS IN CANCER BIOLOGY
(2022)
Review
Medicine, General & Internal
Dimitrios Goutas, Stamatios Theocharis, Gerasimos Tsourouflis
Summary: HDACs play important roles in tumorigenesis and tumor progression, showing potential as therapeutic targets in cancer treatment. However, their clinical significance as biomarkers in cancer is not fully elucidated. This study aims to emphasize the clinical significance of HDAC isoform expression in different tumor types and their correlations with clinicopathological parameters and patient outcomes.
Review
Biochemistry & Molecular Biology
Svetlana Demyanenko, Valentina Dzreyan, Svetlana Sharifulina
Summary: Cerebral ischemia is the second leading cause of death worldwide, requiring multimodal stroke therapy. Histone deacetylase inhibitors have shown to be effective in protecting the brain from ischemic damage by inducing neurogenesis and angiogenesis in damaged brain areas, promoting functional recovery after stroke.
Review
Obstetrics & Gynecology
Marina Ilicic, Tamas Zakar, Amy Gregson, Waleed M. Hussein, Roger Smith, Jonathan W. Paul
Summary: The article summarizes the crucial role of myometrial phenotypic transformation during pregnancy to facilitate childbirth, and the involvement of protein acetylation in this process. Studies show that histone deacetylase inhibitors have significant relaxation effects on pregnant human myometrium.
REPRODUCTIVE SCIENCES
(2022)
Article
Chemistry, Medicinal
Yuqi Jiang, Jie Xu, Kairui Yue, Chao Huang, Mengting Qin, Dongyu Chi, Qixin Yu, Yue Zhu, Xiaohan Hou, Tongqiang Xu, Min Li, C. James Chou, Xiaoyang Li
Summary: The study focused on modifying HDAC inhibitors to deactivate the Michael reaction in order to improve their potency. Compound 11h showed significant improvements in both HDAC inhibitory activity and cell-based antitumor assay, demonstrating potential for clinical application and efficacy against AML.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Medicine, Research & Experimental
Zhengke Wang, Yu Tina Zhao, Ting C. Zhao
Summary: Cardiovascular diseases are the leading cause of mortality worldwide. Histone deacetylases (HDACs) play a crucial role in epigenetic regulation of genetic transcription during stress or pathological conditions, making them a potential target for treating cardiac diseases. Further understanding HDACs can lead to new therapeutic strategies in cardiovascular disorders.
EXPERIMENTAL BIOLOGY AND MEDICINE
(2021)
Article
Chemistry, Medicinal
Yawen Yang, Qingqing Liu, Xinyi Wang, Shaohua Gou
Summary: A series of novel histone deacetylase (HDAC) inhibitors derived from 3-(benzazol-2-yl)quinoxaline derivatives were designed and synthesized using a pharmacophore fusion strategy. In vitro studies demonstrated that most of the synthesized compounds exhibited significant anti-proliferative activity. Among them, compound 10c showed the highest cytotoxicity in HCT-116 cells with an IC50 value of 0.91 μM, surpassing Vorinostat (5.66 μM). Further investigation revealed that compound 10c up-regulated the acetylation levels of H3 and alpha-tubulin, inhibited Topo I, and induced the release of apoptotic biomarkers, highlighting its potential as a promising anti-cancer HDAC inhibitor.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Immunology
Mahdieh Mehrpouri, Atieh Pourbagheri-Sigaroodi, Davood Bashash
Summary: This article outlines the role of epigenetic modulations, particularly histone deacetylases, in hematologic malignancies and their therapeutic potential. Research suggests that HDACs play a significant role in hematopoiesis and the development of blood cancers.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2021)
Review
Oncology
Fengyi Guo, Hongjing Wang
Summary: This review summarizes the classification and mechanisms of action of histone deacetylase and the clinical application of their inhibitors in ovarian cancer. Histone deacetylase inhibitors show promising potential as anti-cancer drugs, and combination therapy with other anticancer drugs for synergistic effects can improve efficacy.
FRONTIERS IN ONCOLOGY
(2022)
Review
Medicine, Research & Experimental
Yu Liu, Xinyi Shen, Mingchang Pang, Zhen Sun, Yongjiang Qian, Wenxin Xue, Zhongqun Wang, Lihua Li
Summary: Atherosclerosis (AS) is the leading cause of death in cardiovascular diseases, and Sirt3, an important histone deacetylase, plays a crucial role in the development and regression of AS by deacetylating mitochondrial proteins in blood vessels and participating in various metabolic activities. Medical research targeting Sirt3 is also actively underway, aiming to provide new insights and intervention strategies for AS.
Article
Immunology
Melanie A. Whitmore, Hong Li, Wentao Lyu, Sharmily Khanam, Guolong Zhang
Summary: The combination of HDACi and DNMTi/HMTi showed a strong synergy in inducing HDP gene expression, and also regulated the expression of tight junction proteins.
FRONTIERS IN IMMUNOLOGY
(2022)
Review
Cell Biology
Nuraqila Mohd Murshid, Faridah Aminullah Lubis, Suzana Makpol
Summary: Epigenetic mechanisms involving histone methylation and acetylation play a crucial role in gene expression and protein function regulation in neuronal cells. Manipulations of these mechanisms have been shown to affect the susceptibility of neurons to degeneration and apoptosis in neurodegenerative disorders.
CELLULAR AND MOLECULAR NEUROBIOLOGY
(2022)
Editorial Material
Oncology
Nuno Tiago Tavares, Rui Henrique, Carmen Jeronimo, Joao Lobo
Summary: Epidrugs, specifically histone deacetylase inhibitors (HDACi), have shown increasing potential in the treatment of testicular germ cell tumours (TGCTs). Recent research identified SINHCAF as a potential oncogene in TGCTs, supporting the use of HDACi and advocating for further preclinical and clinical studies with these compounds.
JOURNAL OF PATHOLOGY
(2023)
Article
Engineering, Biomedical
Henry F. Duncan, Yoshifumi Kobayashi, Michaela Kearney, Emi Shimizu
Summary: This opinion-led review paper emphasizes the importance of innovative translational research in vital-pulp-treatment (VPT) and discusses the challenges in implementing evidence in clinics. The traditional dentistry approach, which is expensive and invasive, lacks a biological perspective. Recent research focuses on developing minimally-invasive biologically-based 'fillings' that preserve dental pulp and shift the paradigm towards smart restorations targeting biological processes. The potential use of histone-deacetylase (HDAC) inhibitors in stimulating pro-regenerative effects and enhancing biomaterial-driven tissue responses in VPT is analyzed in this article.
BIOACTIVE MATERIALS
(2023)