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
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
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
Pharmacology & Pharmacy
Ekta Shirbhate, Ravichandran Veerasamy, Sai H. S. Boddu, Amit K. Tiwari, Harish Rajak
Summary: One significant obstacle in cancer treatment is the decrease in drug efficacy and occurrence of adverse effects. Oncolytic viruses (OVs) have gained interest as a potential method to treat cancer due to their specificity for cancerous tissue and reduced likelihood of adverse effects. Clinical trials have shown that OVs have an acceptable safety profile and are effective in treating certain types of cancer, despite their limited availability. However, further advancements are needed to enhance tumor permeation and improve virus delivery in order to make oncolytic virotherapy more effective.
DRUG DISCOVERY TODAY
(2022)
Review
Biochemistry & Molecular Biology
Long Xu, Xiaoyu Yan, Jian Wang, Yuanxin Zhao, Qingqing Liu, Jiaying Fu, Xinyi Shi, Jing Su
Summary: This article provides an overview of ovarian cancer metastasis and the dysregulated expression of HDACs in ovarian cancer. It discusses the roles of HDACs in the regulation of ovarian cancer metastasis and highlights the importance of developing compounds that target HDACs in the future of ovarian cancer therapy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Multidisciplinary Sciences
Hong Lei, Seth Haney, Christopher M. Jernigan, Xiaojiao Guo, Chelsea N. Cook, Maxim Bazhenov, Brian H. Smith
Summary: This study demonstrates that honey bees have the ability to differentiate between familiar and novel odors and exhibit different responses. This suggests the presence of mechanisms for novelty detection in early sensory processing.
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
Biochemistry & Molecular Biology
Svetlana Demyanenko, Svetlana Sharifulina
Summary: HDAC and HAT play crucial roles in regulating cell functions through acetylating/deacetylating histones and non-histone proteins, impacting cell survival, death, and other processes. The effects of stroke on non-histone protein acetylation/deacetylation in brain cells are still poorly understood, but HDAC inhibitors have shown promise in protecting the brain from ischemic damage. The roles of different HDAC isoforms in brain cell survival and death after stroke remain controversial.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Chemistry, Medicinal
Xin-Hui Zhang, Qin-Ma, Hui-Pan Wu, Mussa Yussuf Khamis, Yi-Han Li, Li-Ying Ma, Hong-Min Liu
Summary: In this translation, the essential role of HDACs in maintaining homeostasis is discussed, with a focus on the unique characteristics and diverse functions of HDAC6. HDAC6 inhibitors have shown promising potential in treating various diseases with reduced toxicity. Progress has been made in defining the crystal structures of HDAC6 catalytic domains, which can inform the development of HDAC6 inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Neurosciences
Heather J. Pribut, Daniela Vazquez, Alice D. Wei, Stephen S. Tennyson, Ian R. Davis, Matthew R. Roesch, Xuan Li
Summary: This study found that overexpression of HDAC5 in the dorsal striatum of rats leads to faster response and more frequent selection of high-value rewards in the first set of trials, but less flexibility in reversing these contingencies in the second set. At the neural level, HDAC5 overexpression in the dorsal striatum increases and decreases the number of cells in the dorsolateral striatum that respond to stimuli and rewards, respectively, and shifts encoding towards cues predicting more immediate rewards.
JOURNAL OF NEUROSCIENCE
(2021)
Article
Chemistry, Physical
Ye Yang, Baichun Hu, Yi Yang, Kaihua Gong, Huibin Wang, Qi Guo, Xinjie Tang, Yujuan Li, Jian Wang
Summary: The study utilized various computational methods to clarify the structural basis of selective inhibition towards HDAC2 over HDAC8 and demonstrated the different binding modes of inhibitors with the two isoforms. The results revealed the diverse interaction patterns of HDAC2 and HDAC8 inhibitors with Zn2+ ions.
PHYSICAL CHEMISTRY CHEMICAL PHYSICS
(2021)
Article
Oncology
Weiyu Dai, Side Liu, Jieming Zhang, Miaomiao Pei, Yizhi Xiao, Jiaying Li, Linjie Hong, Jianjiao Lin, Jing Wang, Xiaosheng Wu, Guangnan Liu, Yaying Chen, Yusi Wang, Zhizhao Lin, Qiong Yang, Fachao Zhi, Guoxin Li, Weimei Tang, Aimin Li, Li Xiang, Jide Wang
Summary: miR-769-5p/miR-769-3p acts as a tumor suppressor in gastric cancer by targeting IGF1R and through the STAT3-IGF1R-HDAC3 complex. Treatment with the HDAC inhibitor SAHA triggers the expression of miR-769-5p/miR-769-3p, leading to inhibition of proliferation and induction of apoptosis in gastric cancer cells.
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
Physiology
Ettore Tiraboschi, Luana Leonardelli, Gianluca Segata, Albrecht Haase
Summary: Insects, particularly bees, have been found to have a significant neuronal response to mechanical stimuli in addition to odors. This study using fast two-photon calcium imaging in honey bees revealed that clean air pulses generate a complex pattern of glomerular activation, providing a code for stimulus intensity and dynamics. The discovery of a dual function in the insect olfactory system gives hope for a better understanding of sensory mechanisms in animals.
FRONTIERS IN PHYSIOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Marta Halasa, Kamila Adamczuk, Grzegorz Adamczuk, Syeda Afshan, Andrzej Stepulak, Marek Cybulski, Anna Wawruszak
Summary: N-ε-lysine acetylation/deacetylation is a common post-translational modification regulated by histone acetyltransferases and histone deacetylases, influencing the properties and functions of histones and non-histone proteins, including transcription factors that alter cell signaling pathways and impact cancer progression. HDACs play a significant role in deacetylating targets, leading to the regulation of proteins involved in cell cycle and apoptosis, ultimately affecting tumor growth, invasion, and drug resistance. This review highlights the clinical importance of epigenetic modifications as a potential therapeutic target in cancer treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)