Review
Cell & Tissue Engineering
Luana Abballe, Evelina Miele
Summary: Cancer stem cells within brain tumors play a crucial role in cancer growth and progression, influencing treatment response and leading to tumor relapse. Reversing cancer epigenome is considered a promising therapeutic strategy in targeting these cells. Epigenetic mechanisms such as DNA methylation, histone modifications, and non-coding RNA can be specifically targeted by epidrugs to combat brain tumor stem-like cells.
WORLD JOURNAL OF STEM CELLS
(2021)
Article
Oncology
Qian Zhao, Shan-Shan Xiong, Can Chen, Hong-Ping Zhu, Xin Xie, Cheng Peng, Gu He, Bo Han
Summary: The authors designed and synthesized a series of compounds with dual inhibitory activity against MDM2 and HDAC, and found that compound 11b exhibited the strongest inhibition against both targets. This compound also showed effective antiproliferative activity towards MCF-7 cells and increased the expression of p53 and Ac-H4. These results suggest that dual inhibition of HDAC and MDM2 may provide a novel and efficient strategy for the discovery of antitumor drugs in the future.
FRONTIERS IN ONCOLOGY
(2022)
Review
Oncology
Robert Jenke, Nina Ressing, Finn K. Hansen, Achim Aigner, Thomas Buch
Summary: Epigenetic changes can drive cancer malignancy, while histone deacetylase inhibitors (HDACis) hold promise as anticancer drugs due to their ability to target multiple pathways relevant to the disease.
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.
Article
Oncology
Margarita E. Neganova, Sergey G. Klochkov, Yulia R. Aleksandrova, Gjumrakch Aliev
Summary: Epigenetic changes associated with histone modifications are important in the emergence and maintenance of various cancer types. Inhibitors of enzymes involved in these modifications are promising for anticancer drug development. This review explores the main features of common histone modifications and their role in malignant neoplasms, discussing strategies for inhibitor development and analyzing the use of multitarget drugs as the most promising strategy.
SEMINARS IN CANCER BIOLOGY
(2022)
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)
Article
Chemistry, Medicinal
Nils Goehringer, Yayi Peng, Bianca Nitzsche, Hannah Biermann, Rohan Pradhan, Rainer Schobert, Marco Herling, Michael Hoepfner, Bernhard Biersack
Summary: The development of new anticancer drugs is essential due to the limitations of current drugs. Histone deacetylases (HDACs) have emerged as promising targets for cancer treatment. SF5-SAHA, a newly synthesized HDAC inhibitor, showed strong inhibition of tumor cell growth and potential for further development as an anticancer drug candidate.
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)
Editorial Material
Oncology
Carlos Jimenez, Lucas Moreno, Miguel F. Segura
Summary: The low immunogenicity of neuroblastoma cells, represented by the low expression of major histocompatibility complex class I, poses a challenge to the development of immunotherapies. Cornel et al. demonstrated that epigenetic modulation of neuroblastoma cells using a histone deacetylase inhibitor can enhance the expression of major histocompatibility complex class I and other immune receptors, enabling their recognition by T- and natural killer cells. These discoveries leverage the aberrant epigenetic landscapes of neuroblastoma and provide a potential solution to overcome a major limitation in neuroblastoma immunotherapy.
MOLECULAR ONCOLOGY
(2023)
Article
Medicine, Research & Experimental
Maria J. Klomp, Lilian van den Brink, Peter M. van Koetsveld, Corrina M. A. de Ridder, Debra C. Stuurman, Clemens W. G. M. Lowik, Leo J. Hofland, Simone U. Dalm
Summary: In vitro experiments showed that HDAC inhibitors had the desired effects. However, there was no significant increase in tumoral DOTA-TATE uptake after HDAC inhibitor treatment in NCI-H69 tumor-bearing animals. The expression levels of tumoral SSTR2 mRNA and/or protein were significantly upregulated after treatment with certain inhibitors. There was a significant inverse correlation between HDAC3 and SSTR2 expression in the studied cell lines.
Article
Chemistry, Physical
Avineesh Singh, Vijay K. Patel, Harish Rajak
Summary: Pyrrole as a connecting unit demonstrates potent anticancer activity against various cancer cell lines. Substitution with different groups influences the activity of the compounds, and further development of novel SAHA analogs with promising anticancer activity can be pursued based on these studies.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Review
Medicine, Research & Experimental
Janice Jacson Mandumpala, Stephin Baby, Antriya Annie Tom, Chandraiah Godugu, Nagula Shankaraiah
Summary: Triple-negative breast cancer (TNBC) is a highly lethal subtype of breast cancer with limited treatment options due to its complexity, drug resistance, and lack of therapeutic targets. Recent studies have shown the importance of epigenetic regulation in TNBC development, with a focus on histone methyltransferases and histone demethylases as potential targets for new targeted therapies in TNBC treatment.
Article
Oncology
Bernhard Biersack, Sibel Polat, Michael Hoepfner
Summary: Histone deacetylases (HDACs) are epigenetic regulators that affect chromatin condensation and cancer proliferation. HDAC inhibitors are promising drugs for cancer treatment. However, there are limitations and resistance issues in clinical application, leading to the search for new HDAC inhibitors. Kinase inhibitors, when used in combination with HDAC inhibitors, show synergistic anticancer effects.
SEMINARS IN CANCER BIOLOGY
(2022)
Review
Medicine, Research & Experimental
Nasreddine El Omari, Learn-Han Lee, Saad Bakrim, Hafiz A. Makeen, Hassan A. Alhazmi, Syam Mohan, Asaad Khalid, Long Chiau Ming, Abdelhakim Bouyahya
Summary: Romidepsin, a natural molecule produced by Chromobacterium violaceum bacterium, has been approved for its anti-cancer effect. It is a selective histone deacetylase (HDAC) inhibitor that modifies histones and epigenetic pathways. This review aims to highlight the specific molecular mechanisms responsible for HDAC inhibition by romidepsin, which can significantly improve the understanding of cancer cell disorders and pave the way for new therapeutic approaches using targeted therapy.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Multidisciplinary Sciences
Wanlin Jiang, Megan E. Block, Chandra S. Boosani
Summary: This study investigates the role of TNF-alpha and IGF-1 in regulating the epigenetic mechanisms that promote VSMCs proliferation, and identifies a novel molecular mechanism involving DNMT1, HDAC10, and HDAC2. Results reveal the inter-dependence of epigenetic mediators in VSMCs proliferation.