Article
Chemistry, Medicinal
Elisabetta Di Bello, Veronica Sian, Giulio Bontempi, Clemens Zwergel, Rossella Fioravanti, Beatrice Noce, Carola Castiello, Stefano Tomassi, Davide Corinti, Daniela Passeri, Roberto Pellicciari, Ciro Mercurio, Mario Varasi, Lucia Altucci, Marco Tripodi, Raffaele Strippoli, Angela Nebbioso, Sergio Valente, Antonello Mai
Summary: After years of research, HDAC inhibitors have been developed and approved by FDA/Chinese FDA for the treatment of cancer and non-cancer diseases. A series of novel compounds have been discovered to be effective anticancer agents, demonstrating selective inhibition of HDACs and inducing cell death and differentiation. These compounds also modulate gene and protein expression related to apoptosis and show potent antiproliferative activity in various cancer cell lines.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Cell Biology
Zhenzhen Jiang, Xiaoli Zheng, Weijia Wang, Liqing Qiu, Lingrong Yang, Mingfeng Jiang, Yuhui Hua
Summary: The study found downregulation of CYP2C9 in human esophageal squamous cell carcinoma. The epigenetic analysis revealed that inhibition of HDAC8 and HDAC1 could increase the expression of CYP2C9. Overexpression of CYP2C9 reduces the invasion and migration ability of ESCC cells.
MOLECULAR AND CELLULAR BIOCHEMISTRY
(2021)
Article
Plant Sciences
Yan Xu, Yuanxin Miao, Botao Cai, Qingping Yi, Xuejun Tian, Qihai Wang, Dan Ma, Qiong Luo, Feng Tan, Yongfeng Hu
Summary: This paper investigates the role of histone deacetylase inhibitors in rice disease resistance. It is found that sodium butyrate treatment significantly enhances rice blast resistance. The global histone acetylation is increased after treatment with the four inhibitors, but at different sites, suggesting different selectivity of these inhibitors. Transcriptomic analysis reveals that many defense-related genes are up-regulated by sodium butyrate treatment.
FRONTIERS IN PLANT SCIENCE
(2022)
Review
Biochemistry & Molecular Biology
Maria Manou, Dimitrios S. Kanakoglou, Theodoros Loupis, Dimitrios M. Vrachnos, Stamatios Theocharis, Athanasios G. Papavassiliou, Christina Piperi
Summary: Salivary gland tumors (SGTs) are a rare and heterogeneous category of tumors with increasing understanding of their molecular mechanisms, poor prognosis, and potential therapeutic options. Genetic and epigenetic factors are involved in their heterogeneity and clinical phenotypes. Histone acetylation/deacetylation, through histone deacetylating factors (HDACs) and selective or pan-HDAC inhibitors (HDACis), plays an active role in the pathobiology of SGTs, suggesting potential treatment options. This article summarizes the molecular and epigenetic mechanisms of SGTs, focusing on the effects of histone acetylation/deacetylation on gene expression and the progress of HDACis in SGT therapy and clinical trials.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Genetics & Heredity
Subramaniam Jayanthi, Michael T. McCoy, Jean Lud Cadet
Summary: Methamphetamine-use disorder is a serious condition that can lead to long-term changes in the brain and gene expression, highlighting the importance of researching the underlying mechanisms.
Review
Medicine, Research & Experimental
M. Janaki Ramaiah, Anjana Devi Tangutur, Rajasekhar Reddy Manyam
Summary: Genetic and epigenetic factors play crucial roles in tumor initiation and progression, with HDAC inhibitors showing promise in inducing tumor suppression by regulating chromatin conformation.
Article
Pharmacology & Pharmacy
Geer Chen, Xiaoyu Zhu, Jiaqi Li, Yao Zhang, Xiaoxuan Wang, Ren Zhang, Xinchen Qin, Xi Chen, Junyi Wang, Weilin Liao, Zongjin Wu, Lu Lu, Weiyu Wu, Haijie Yu, Lijuan Ma
Summary: Alterations in histone modification have been shown to be related to cancer development and progression. Celastrol, a Chinese herbal compound, exhibits potent anti-tumor effects through multiple signaling pathways. This study demonstrates that histone modifications, especially histone acetylation associated with the NuA4 histone acetyltransferase complex, are involved in the anti-proliferation actions of celastrol. Combination therapy with celastrol and histone deacetylase inhibitors (HDACi) synergistically suppresses cancer cell proliferation. The results suggest that the combination of celastrol and HDACi could be a potential novel therapeutic approach for lung cancer patients.
PHARMACOLOGICAL RESEARCH
(2022)
Review
Biochemistry & Molecular Biology
Jinkal Modi, Abhishek Roy, Anjan K. Pradhan, Amit Kumar, Sarmistha Talukdar, Praveen Bhoopathi, Santanu Maji, Padmanabhan Mannangatti, Daniel Sanchez de la Rosa, Jiong Li, Chunqing Guo, Mark A. Subler, Jolene J. Windle, Webster K. Cavenee, Devanand Sarkar, Xiang-Yang Wang, Swadesh K. Das, Luni Emdad, Paul B. Fisher
Summary: MDA-7/IL-24 is a potent tumor suppressor with multiple functions, including inhibition of tumor growth, invasion, angiogenesis, and metastasis, induction of bystander antitumor activity, and synergy with conventional cancer therapeutics.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Flore Nardella, Ludovic Halby, Irina Dobrescu, Johanna Viluma, Corentin Bon, Aurelie Claes, Veronique Cadet-Daniel, Ambre Tafit, Camille Roesch, Elie Hammam, Diane Erdmann, Melissa Mairet-Khedim, Roger Peronet, Salah Mecheri, Benoit Witkowski, Artur Scherf, Paola B. Arimondo
Summary: The newly developed derivatives combining pan-histone deacetylase inhibitor with DNA methyltransferase inhibitor show superior activity in treating malaria and potent inhibition against human HDAC6. These compounds are fully active against multidrug-resistant Plasmodium and offer a cost-effective alternative to current failing antimalarial therapy.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biology
Alicia Tapias, David Lazaro, Bo-Kun Yin, Seyed Mohammad Mahdi Rasa, Anna Krepelova, Erika Kelmer Sacramento, Paulius Grigaravicius, Philipp Koch, Joanna Kirkpatrick, Alessandro Ori, Francesco Neri, Zhao-Qi Wang
Summary: The study reveals the importance of TRRAP for neuroprotection and the network connecting TRRAP, HAT, and SP1 in regulating microtubule dynamics.
Article
Immunology
Mahdieh Mehrpouri, Atieh Pourbagheri-Sigaroodi, Davood Bashash
Summary: This article outlines the role of epigenetic modulations, particularly histone deacetylases, in hematologic malignancies and their therapeutic potential. Research suggests that HDACs play a significant role in hematopoiesis and the development of blood cancers.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2021)
Article
Cell Biology
Maria R. Pozo, Gantt W. Meredith, Emilia Entcheva
Summary: The epigenetic landscape and the responses to pharmacological epigenetic regulators in each human are unique. HDAC inhibitors (HDACi) are widely used in the treatment of cancer and immune diseases. However, the effects of these epigenetic modulators on cardiac tissue are not well understood. hiPSC-CM technology can be used as a high-throughput platform to study the functional electrophysiological responses of the heart and quantify the responses to HDACi.
Article
Cell Biology
Mei Wu, Zehong Huang, Wenfang Huang, Mengyu Lin, Weifeng Liu, Kexuan Liu, Cai Li
Summary: This study investigates the role of microRNA (miR)-124-3p in sepsis-induced myocardial injury and identifies its mechanism of action through targeted regulation of SP1 to alleviate inflammation, oxidative stress, and apoptosis, thus improving myocardial injury in septic rats.
CELL DEATH DISCOVERY
(2022)
Article
Biochemistry & Molecular Biology
Michela Giuliano, Claudia Pellerito, Adriana Celesia, Tiziana Fiore, Sonia Emanuele
Summary: Organotin(IV) compounds are a class of non-platinum metallo-conjugates with antitumor properties. Among them, triorganotin(IV) butyrate (BT2) shows high efficacy in colon cancer cells by inducing G2/M cell cycle arrest, ER stress, and apoptotic cell death. Furthermore, BT2 can decrease histone acetylation levels and prevent acetylation induced by other HDAC inhibitors, suggesting its potential as an epigenetic modulator in colon cancer treatment.
Article
Genetics & Heredity
Eliza Mari Kwesi-Maliepaard, Muddassir Malik, Tibor van Welsem, Remco van Doorn, Maarten H. Vermeer, Hanneke Vlaming, Heinz Jacobs, Fred van Leeuwen
Summary: The therapeutic effect of commonly used pan-HDAC inhibitors in CTCL cells may rely on downstream effects that are unrelated to the regulation of DOT1L.
FRONTIERS IN GENETICS
(2022)