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)
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)
Article
Biochemistry & Molecular Biology
Wenli Fan, Lin Zhang, Xuejiang Wang, Haiyong Jia, Lei Zhang
Summary: In this study, pharmacophores of phenanthridine were incorporated into HDAC inhibitors, and fatty and aromatic linkers were evaluated for solubility and activity. Compounds with aromatic linker showed better activities than those with fatty linker. Molecule Fb-4 exhibited promising anticancer potency by inducing G2/M phase arrest and apoptosis in MCF-7 cells, suggesting its potential as a lead compound for further drug design.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Davide Moi, Andrea Citarella, Davide Bonanni, Luca Pinzi, Daniele Passarella, Alessandra Silvani, Clelia Giannini, Giulio Rastelli
Summary: In this study, two potent and selective HDAC6 inhibitors were obtained through chemoinformatic analysis. The newly discovered aminotriazole-based compounds showed higher inhibitory activity and have the potential to be optimized as anticancer compounds.
Article
Oncology
Hao Wang, Lei Shi, Zhimin Wang
Summary: The research demonstrated that the structurally modified DMC-HA effectively inhibited human glioblastoma U87 cells, induced apoptosis, and increased histone H3 acetylation levels. Pharmacokinetic studies indicated acceptable pharmacokinetic properties for DMC-HA in vivo, suggesting its potential for further development as a chemotherapeutic drug.
FRONTIERS IN ONCOLOGY
(2021)
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)
Article
Chemistry, Medicinal
Xing-Jie Zhang, Ming-Hui Liu, Yu-Sha Luo, Gui-Yan Han, Zhi-Qiang Ma, Fei Huang, Yuan Wang, Zhen-Yuan Miao, Wan-Nian Zhang, Chun-Quan Sheng, Jian-Zhong Yao
Summary: The synthesis of novel cytotoxic chlorin-based derivatives as dual photosensitizers and histone deacetylase inhibitors was investigated for biological activity. Compound 15e showed high phototoxicity, induced cell apoptosis in multiple organelles, and could be applied as a potential dual cytotoxic drug for PDT and chemotherapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
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
Chemistry, Medicinal
Hualong Mo, Ruiqiang Zhang, Yajun Chen, ShuTing Li, Yao Wang, Wenbo Zou, Qiman Lin, Deng-Gao Zhao, Yarong Du, Kun Zhang, Yan-Yan Ma
Summary: Compound 21 is an effective anticancer agent that inhibits tumor growth by inhibiting autophagy and inducing cell apoptosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Kai-Cheng Hsu, Jung-Chun Chu, Hui-Ju Tseng, Chia- Liu, Hao-Ching Wang, Tony Eight Lin, Hong-Sheng Lee, Ling-Wei Hsin, Andrew H-J Wang, Chien-Huang Lin, Wei-Jan Huang
Summary: The study showed that modifying the acridine ring with phenothiazine derivatives can effectively inhibit the activity of class II HDACs, with compound 4f exhibiting the strongest inhibitory effect and promoting neurite outgrowth.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(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)
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, Multidisciplinary
Tianyi Zhang, Xiaoyan Zhao, Xiangpei Sun, Wei Tian, Chongqing Wang, Mingping Wang, Yi Zhang, Xin Chen, Canhui Zheng
Summary: This study aimed to discover novel HDAC6 selective inhibitors, and a new class of compounds with excellent inhibitory activities and selectivity was obtained through structural optimization of the previously reported inhibitor 7g. These compounds showed inhibitory effects on HDAC6, a protein associated with diseases such as cancer, and may have lower toxicity to normal cells and tissues.
JOURNAL OF SAUDI CHEMICAL SOCIETY
(2022)
Article
Biochemistry & Molecular Biology
Simin Sun, Wenwen Zhao, Yongliang Li, Ziwei Chi, Xixi Fang, Qiang Wang, Zhiwu Han, Yepeng Luan
Summary: The study focused on the design and synthesis of a series of HDAC inhibitors, identifying compound 6h as a promising candidate with potent antitumor effects. Compound 6h exhibited high cytotoxicity against various cancer cell lines, arrested cell cycle, induced apoptosis, and demonstrated anti-migration and anti-angiogenesis activities. Additionally, compound 6h increased the expression of acetylated alpha-tubulin and acetylated histone H3, fitting well into the active sites of HDAC2 and 6, suggesting its potential for further preclinical studies.
BIOORGANIC CHEMISTRY
(2021)