Article
Hematology
Takeshi Harada, Hiroto Ohguchi, Asuka Oda, Michiyasu Nakao, Jumpei Teramachi, Masahiro Hiasa, Ryohei Sumitani, Masahiro Oura, Kimiko Sogabe, Tomoko Maruhashi, Mamiko Takahashi, Shiro Fujii, Shingen Nakamura, Hirokazu Miki, Kumiko Kagawa, Shuji Ozaki, Shigeki Sano, Teru Hideshima, Masahiro Abe
Summary: Histone deacetylase 1 (HDAC1) regulates the expression of transcription factor IRF4 and survival mediator PIM2 kinase in multiple myeloma (MM) cells. Inhibition of HDAC1 reduces the expression of IRF4 and PIM2, and decreases IRF4 transcription through histone hyperacetylation. External stimuli such as BM stromal cells and interleukin-6 (IL-6) upregulate PIM2, attenuating the cytotoxic effects of HDAC1 inhibitors.
Article
Cell Biology
Yong Wang, Fen Liu, Chen Fang, Liyao Xu, Lin Chen, Zeyao Xu, Jiaquan Chen, Wei Peng, Biqi Fu, Yong Li
Summary: The combination treatment of RAPA and SAHA significantly enhances the inhibitory effect of radiotherapy on NSCLC, primarily by modulating the expression of DNA damage proteins and increasing radiotherapy sensitivity. This combined therapy also effectively inhibits tumor growth in the A549 xenograft model.
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
Hematology
Shirong Li, Jing Fu, Jun Yang, Huihui Ma, Divaya Bhutani, Markus Y. Mapara, Christophe Marcireau, Suzanne Lentzsch
Summary: In multiple myeloma with RAS mutations, GCK was identified as a novel therapeutic target. Targeting GCK showed high effectiveness in RAS(Mut) MM cells, while GCK kinase activity was critical for regulating MM cell proliferation and survival. GCK inhibitors might represent an alternative therapy to overcome immunomodulatory drug resistance in MM.
Article
Biochemistry & Molecular Biology
Olga O. Gnedina, Alisa Morshneva, Elena Skvortsova, Maria Igotti
Summary: Histone deacetylase inhibitors (HDACis) can interfere with DNA damage response, enhancing the efficacy of genotoxic agents in cancer treatment, without harming normal cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(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
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
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.
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
Biochemistry & Molecular Biology
Xiaocui Shi, Yajuan Yin, Xuwen Guo, Mei Liu, Fangfang Ma, Li Tian, Mingqi Zheng, Gang Liu
Summary: Calcium overload plays a crucial role in the pathogenesis of myocardial ischemia-reperfusion (I/R) damage, leading to mitochondrial impairment and apoptosis of cardiomyocytes. Sub-eroylanilide hydroxamic acid (SAHA), a histone deacetylases inhibitor with modulatory capacity on Na+-Ca2+ exchanger (NCX), has been shown to have protective potential against cardiac remodeling and injury. The present research explored the modulation of NCX-Ca2+-CaMKII by SAHA in myocardial I/R damage. The results indicated that SAHA treatment alleviated myocardial cell apoptosis and mitochondrial dysfunction resulting from myocardial I/R impairment, and contributed to myocardial function recovery by inhibiting the NCX-Ca2+- CaMKII pathway.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
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
Qinglang Mei, Xiaohan Xu, Danling Gao, Yuting Xu, Jinbo Yang
Summary: This study demonstrates that LAQ upregulates the Notch signaling pathway in solid tumor cell lines at the molecular level. It also shows that the combination of LAQ and a Notch signaling pathway inhibitor has a synergistic effect in inhibiting solid tumor cell line proliferation in vitro and significantly inhibits tumor cell growth in vivo using an allograft tumor model. Inhibition of the Notch signaling pathway provides a valuable strategy for enhancing solid tumor sensitivity to LAQ.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(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.
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)