Review
Pharmacology & Pharmacy
Hae Jin Kee, Inkyeom Kim, Myung Ho Jeong
Summary: This article provides an overview of the pathogenesis of hypertension, current anti-hypertensive drugs, and the need for novel drugs. It focuses on the role and regulatory mechanisms of HDACs in hypertension and discusses the progress in developing HDAC inhibitors as potential therapeutic targets.
BIOCHEMICAL PHARMACOLOGY
(2022)
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.
Article
Agricultural Engineering
Xuefeng Lu, Tae Kyung Hyun
Summary: Post-translational histone modifications, such as histone acetylation, play key roles in regulating gene expression in plant growth, development, and stress responses. The research found that HDAC inhibitors led to hyperacetylation of histone H3, enhancing MeJA-induced ginsenoside production in ginseng adventitious roots. Additionally, the study identified specific PgHDACs that may serve as crucial factors in controlling MeJA-induced ginsenoside production.
INDUSTRIAL CROPS AND PRODUCTS
(2021)
Review
Oncology
Amandine Badie, Christian Gaiddon, Georg Mellitzer
Summary: Our understanding of the identity of many cancers has greatly increased in recent years, leading to progress in early detection and treatment options. However, gastric cancer remains poorly treated with low survival rates. The lack of possibilities for early detection and the variations between tumors of gastric cancer patients are major challenges. Histone Deacetylases (HDACs) have been identified to be potentially related to gastric cancer. In this review, we summarize the current knowledge on the role of HDACs in gastric cancer development and their potential as early detection markers and targets for new treatment options.
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
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)
Article
Multidisciplinary Sciences
William Villiers, Audrey Kelly, Xiaohan He, James Kaufman-Cook, Abdurrahman Elbasir, Halima Bensmail, Paul Lavender, Richard Dillon, Borbala Mifsud, Cameron S. Osborne
Summary: The PML-RARA gene fusion is the characteristic driver of Acute Promyelocytic Leukaemia (APL) and is known to bind to the genome. Here, the authors characterise the impact of PML-RARA on gene regulation in APL cell lines and patient samples using transcriptomics, epigenomics, and machine learning.
NATURE COMMUNICATIONS
(2023)
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
Chemistry, Physical
Jinjiao Dong, Xinyue Zhu, Wei Yu, Xiaotong Hu, Yiwen Zhang, Kan Yang, Zhihao You, Zhenming Liu, Xiaoqiang Qiao, Yali Song
Summary: A series of pyrazolo [3,4-d]pyrimidine-based dual HDAC/Topo II inhibitors were synthesized, showing excellent dual inhibitory activities against HDAC and Topo II. These compounds displayed potent cytotoxicity in cancer cell lines and inhibited the migration of MCF-7 cells. Further studies revealed that compounds 12 and 24 promoted apoptosis in MCF-7 cells and showed significant interaction with active sites of HDAC and Topo II.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Oncology
Jia Yin, Chao-Ling Wan, Ling Zhang, Hao Zhang, Lian Bai, Hai-Xia Zhou, Ming-Zhu Xu, Li-Yun Chen, Chong-Sheng Qian, Hui-Ying Qiu, Su-Ning Chen, Xiao-Wen Tang, De-Pei Wu, Yan-Ming Zhang, Ai-Ning Sun, Sheng-Li Xue
Summary: The study investigated the role of chidamide, decitabine plus priming regimen in the salvage treatment of relapsed/refractory acute myeloid leukemia. The CDIAG regimen showed good antileukemia activity in these patients with acceptable adverse events.
FRONTIERS IN ONCOLOGY
(2021)
Article
Chemistry, Medicinal
Mengmiao Zhao, Kan Yang, Xinyue Zhu, Tian Gao, Wei Yu, Han Liu, Zhihao You, Zhenming Liu, Xiaoqiang Qiao, Yali Song
Summary: In this study, novel compounds containing pyrimido[5,4-b]indole and pyrazolo[3,4-d]pyrimidine motifs were synthesized as dual Topo II/HDAC inhibitors. The MTT assay showed potential antiproliferative activity of these compounds against cancer cell lines and low cytotoxicity on normal cell line. Compound 7d was identified as a Topo II poison and compounds 7d and 8d demonstrated apoptosis promotion and migration inhibition in MCF-7 cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Oncology
Jason Lin, Shang-Chuen Wu
Summary: This review examines the role of protein serotonylation in transcriptional regulation, its potential impact on the epigenetic landscape, and its implications in lung and other types of cancer. The review discusses the mechanistic details of serotonylation and its connections to the epigenome, as well as the role of transglutaminase 2, in order to guide the development of optimized histone deacetylase inhibitor designs or combination therapies for cancer treatment.
Review
Cell Biology
Iason Psilopatis, Kleio Vrettou, Florian Nima Fleckenstein, Stamatios Theocharis
Summary: Endometriosis is a chronic disorder that affects many women globally. Histone deacetylases (HDACs) play a role in gene transcription by regulating chromatin relaxation. This comprehensive review examines the impact of histone modifications and therapeutic targeting, specifically focusing on HDACs and their inhibitors in endometriosis. The five most studied HDAC enzymes, HDAC1, HDAC2, HDAC3, Sirtuin 1, and Sirtuin 3, have been found to influence the pathophysiology of endometriosis. Both established and novel HDACIs show promise as effective anti-endometriotic drugs. Overall, histone modifications and therapeutic targeting have a significant impact on endometriosis.
Article
Immunology
Martina Mazzocchi, Susan R. Goulding, Noelia Morales-Prieto, Tara Foley, Louise M. Collins, Aideen M. Sullivan, Gerard W. O'Keeffe
Summary: The peripheral administration of Class IIa-specific HDIs may have neuroprotective effects in Parkinson's disease.
BRAIN BEHAVIOR AND IMMUNITY
(2022)
Article
Biochemistry & Molecular Biology
Yiming Chen, Lihui Zhang, Lin Zhang, Qixiao Jiang, Lei Zhang
Summary: Through structural modification, a HDAC inhibitor (I13) with high anticancer activity was discovered, showing promising inhibitory and antiproliferative potencies in in vitro investigations and cancer cell screenings. The compound also demonstrated potential for inhibiting tumor growth in animal models.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
