Article
Biochemistry & Molecular Biology
Doan Minh Sang, Ik Ho Na, Duong Tien Anh, Do Thi Mai Dung, Nguyen Thi Thu Hang, Nguyen T. Phuong-Anh, Pham-The Hai, Dao Thi Kim Oanh, Truong Thanh Tung, Soo Jung Lee, Joo Hee Kwon, Jong Soon Kang, Sang-Bae Han, Dinh Thi Thanh Hai, Nguyen-Hai Nam
Summary: In this study, we designed, synthesized, and evaluated novel (E)-3-(3-oxo-4-substituted-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-N-hydroxypropenamides targeting histone deacetylases. The synthesized compounds were tested for cytotoxicity, HDAC inhibitory activity, anticancer activity, and their effects on cell cycle and apoptosis. Our findings showed that compounds 7 e-f were the most active HDAC inhibitors and had good anticancer activity. Docking assays revealed the binding mode and selectivity of compound 7 f towards 8 HDAC isoforms.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Chemistry, Medicinal
Bartosz Bieszczad, Damian Garbicz, Marta Switalska, Marta K. Dudek, Dawid Warszycki, Joanna Wietrzyk, Elzbieta Grzesiuk, Adam Mieczkowski
Summary: In this study, a library of 19 analogues of Vorinostat was developed and tested for their HDAC inhibition and cytotoxic effects on cancer and normal cell lines. Three compounds based on dibenzo[b,f]azocin-6(5H)-one, 11,12-dihydrodibenzo[b,f]azocin-6(5H)-one, and benzo[b]naphtho[2,3-f][1,5]diazocine-6,14(5H,13H)-dione scaffolds showed better HDAC inhibition and lower IC50 values in leukemic and lymphoma cell lines compared to Vorinostat. These compounds exhibited higher activity and selectivity against specific cancer cell lines and a correlation between HDAC inhibition and cytotoxic effects was observed.
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
Food Science & Technology
Muthu Thiruvengadam, Umadevi Subramanian, Baskar Venkidasamy, Prabhu Thirupathi, Ramkumar Samynathan, Mohammad Ali Shariati, Maksim Rebezov, Ill-Min Chung, Kannan R. R. Rengasamy
Summary: Understanding the gut microbiota has become crucial in maintaining human body's homeostasis and preventing disease development. Short-chain fatty acids, produced by gut microbiota fermentation of dietary fiber, play a significant role in modulating the tumor environment and binding to carcinogens for elimination. The gut microbiota may offer new approaches for cancer therapy in the future.
CRITICAL REVIEWS IN FOOD SCIENCE AND NUTRITION
(2023)
Article
Food Science & Technology
Lijin Song, Qinghua Sun, Haonan Zheng, Yiming Zhang, Yujing Wang, Shuangjiang Liu, Liping Duan
Summary: The potential probiotic Roseburia hominis shows anti-neuroinflammatory effects by inhibiting microglial activation and reducing proinflammatory cytokines in the brain. Treatment with propionate or butyrate also leads to decreased neuroinflammation. This study suggests that R. hominis could be a potential psychoprobiotic to reduce neuroinflammation.
MOLECULAR NUTRITION & FOOD RESEARCH
(2022)
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
Biochemistry & Molecular Biology
Pasquale Linciano, Rosaria Benedetti, Luca Pinzi, Fabiana Russo, Ugo Chianese, Claudia Sorbi, Lucia Altucci, Giulio Rastelli, Livio Brasili, Silvia Franchini
Summary: HDAC inhibitors play a significant role in cancer treatment, but their lack of selectivity is a major drawback. Researchers have explored novel linker chemotypes to achieve selective inhibition of different HDAC isoforms. Through in vitro tests and docking calculations, it was found that some candidates could selectively inhibit HDAC1 or HDAC6.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Anu R. Melge, Shraddha Parate, Keechilat Pavithran, Manzoor Koyakutty, C. Gopi Mohan
Summary: The design of unique hybrid molecules combining the pharmacophores of clinically approved BCR-ABL inhibitor and HDAC inhibitor showed promising results in overcoming drug-resistance in CML cells. The virtual screening and in vitro studies revealed the potential of the hybrid molecules in inhibiting BCR-ABL and HDAC activity.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2022)
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)
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
Chemistry, Medicinal
Xiaopeng Peng, Jingxuan Chen, Ling Li, Zhiqiang Sun, Jin Liu, Yichang Ren, Junli Huang, Jianjun Chen
Summary: The novel dual HDAC3/tubulin inhibitor compound 15c showed high potency and selectivity, with excellent antiproliferative effects against various cancer cell lines and significant in vivo antitumor efficacy in a melanoma tumor model. In addition, 15c demonstrated low cardiotoxicity and no nephro-/hepatotoxicity, making it a promising potential anticancer agent.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Editorial Material
Microbiology
Tom Boissavy, Dante Rotili, Thomas Mouveaux, Emmanuel Roger, El Moukthar Aliouat, Christine Pierrot, Sergio Valente, Antonello Mai, Mathieu Gissot
Summary: Toxoplasmosis is a significant health issue for immune-deficient individuals and newborns of infected mothers. New compounds with potent anti-parasitic activity have been discovered, which can serve as therapeutic targets for the treatment of toxoplasmosis.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)
Review
Chemistry, Medicinal
Yi-Min Liu, Jing-Ping Liou
Summary: HDAC inhibitors have been widely studied and used as a strategy to reverse aberrant epigenetic changes associated with cancer. Recently, the combination use of HDAC inhibitors with other drugs has shown superior efficacy in clinical trials. Hence, there is a need for the development of new anticancer treatments and therapeutic regimens.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2023)
Article
Chemistry, Physical
Negar Omidkhah, Farzin Hadizadeh, Khalil Abnous, Razieh Ghodsi
Summary: A series of quinoline-based benzamide derivatives were designed and synthesized as HDAC inhibitors and anticancer agents. The synthesized compounds showed cytotoxic activity against several human cancer cell lines, with the highest cytotoxicity observed in colorectal cancer and lung cancer cells. Compounds with a methyl group at position 2 of the quinoline ring exhibited better cytotoxicity compared to those with an aryl group. The most potent cytotoxic compounds also displayed strong enzyme inhibitory activity.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Tran Khac Vu, Nguyen Thi Thanh, Nguyen Van Minh, Nguyen Huong Linh, Nguyen Thi Phuong Thao, Truong Thuc Bao Nguyen, Doan Thi Hien, Luu Van Chinh, Ta Hong Duc, Lai Duc Anh, Pham-The Hai
Summary: The study aimed to develop novel HDAC inhibitors with potential cytotoxicity against cancer cell lines, and found that compounds bearing conjugated quinazolinone scaffolds showed increased potency in terms of cytotoxicity against MCF-7 cell line compared to SAHA.
MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
M. Manal, K. Manish, D. Sanal, A. Selvaraj, V. Devadasan, M. J. N. Chandrasekar
SAR AND QSAR IN ENVIRONMENTAL RESEARCH
(2017)
Review
Biochemistry & Molecular Biology
M. J. Nanjan, Manal Mohammed, B. R. Prashantha Kumar, M. J. N. Chandrasekar
BIOORGANIC CHEMISTRY
(2018)
Article
Chemistry, Medicinal
Swathi Krishna, Byran Gowramma, Manal Mohammed, Rajagopal Kalirajan, Lakshman Kaviarasan, Thaggikuppe Krishnamurthy Praveen
LETTERS IN DRUG DESIGN & DISCOVERY
(2020)
Correction
Biochemistry & Molecular Biology
Mohamed Marzouk, Shimaa M. Khalifa, Amal H. Ahmed, Ahmed M. Metwaly, Hala Sh. Mohammed, Hanan A. A. Taie
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Gerardo Andres Libreros-Zuniga, Danilo Pava e Pavao, Vinicius de Morais Barroso, Nathalya Cristina de Moraes Roso Mesquita, Saulo Fehelberg Pinto Braga, Glaucius Oliva, Rafaela Salgado Ferreira, Kelly Ishida, Marcio Vinicius Bertacine Dias
Summary: Tuberculosis is a major global cause of death, and the emergence of drug-resistant strains has increased the burden of this disease. New alternative therapies are constantly needed, and recent research has identified small molecules as potential inhibitors of Ldts in M. tuberculosis, which have antimycobacterial activity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xiao-Dong Wang, Yong-Si Liu, Ming-Hao Hu
Summary: In this study, a selffolded fluorescent probe was designed to selectively illuminate G4s by unfolding its intramolecular aggregation mediated by G4 binding. This probe showed more controllable background emission and promising ability to track G4 forming dynamics compared to previous disaggregation-induced emission (DIE) probes.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Xiang, Zhuo Yuan, Qichuan Deng, Linshen Xie, Dongke Yu, Jianyou Shi
Summary: This review provides a brief description of the diagnosis, pathogenesis, and potential therapeutic inhibitors for renal fibrosis. Currently, there are no clear therapeutic targets or drugs for renal fibrosis; however, some natural products may have potential efficacy for treating renal fibrosis.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Simone Giovannuzzi, Anna Nikitjuka, Bruna Rafaela Pereira Resende, Michael Smietana, Alessio Nocentini, Claudiu T. Supuran, Jean-Yves Winum
Summary: Boron-based compounds have been extensively studied in medicinal chemistry, playing a crucial role in designing small molecule drugs for various diseases. Boron is particularly valuable in developing inhibitors for metalloenzymes carbonic anhydrases, and it can modulate ligand recognition ability and selectivity. Recent advancements have led to the discovery of novel boron-based inhibitors that can inhibit carbonic anhydrases through a Lewis acid-base mechanism. Further research is needed to fully explore the potential of boron-based inhibitors and advance their clinical applications.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xinxin Liu, Lei Chen, Ze Chen
Summary: This study developed a nanostructured photosensitizer loaded with oxygen-throttling drug and demonstrated its enhanced cytotoxicity against tumor cells under hypoxic conditions. Animal experiments showed the enhanced tumor targeting capability of the photosensitizer and its inhibitory effect on tumor growth.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Shuai Jiang, Wen-Yan Li, Zai-Feng Yuan, Qin-Shi Zhao
Summary: This study isolated two new dimeric Lycopodium alkaloids and twelve previously undescribed Lycopodium alkaloids from Lycopodiastrum casuarinoides. The structures of these compounds were determined and their inhibitory activities on the Cav3.1 channel were evaluated.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yan Yang, Dong-Xiao Yan, Rui-Xue Rong, Bing-Ye Shi, Man Zhang, Jing Liu, Jie Xin, Tao Xu, Wen-Jie Ma, Xiao-Liu Li, Ke-Rang Wang
Summary: In this study, a series of nucleolar fluorescent probes based on naphthalimide derivatives were designed and synthesized, which could achieve clear nucleolar staining in living cells. The results showed that these probes exhibited good targeting to the cell nucleolus and could bind to RNA and enhance fluorescence. This has positive implications for the diagnosis and treatment of nucleolus-related diseases.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yongxi Dong, Fang Wang, Jinlan Wen, Yongqing Mao, Shanhui Zhang, Tiemei Long, Zhangxiang Yang, Lei Li, Jiquan Zhang, Li Dong, Gang Liu, Jianwei Xu
Summary: The hybrid molecules of Scutellarein and Tertramethylpyrazine show excellent neuroprotective and antiplatelet effects in the treatment of ischemic stroke. Compound 1e is particularly effective, enhancing cell membrane permeability and inhibiting cell uptake, as well as significantly reducing cerebral infarction volume.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Chen, Yuanyuan Ying, Jonathan Lalsiamthara, Yuheng Zhao, Saber Imani, Xin Li, Sijing Liu, Qingjing Wang
Summary: This paper examines the role and metabolic regulation of NAD+ in bacteria, highlighting its impact on physiology and virulence. It explores enzymes associated with NAD+ metabolism as potential targets for antibacterial drugs and vaccine candidates. Additionally, it scrutinizes the medical potential of NAD+ and provides insights for its application in biomedicine.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Jon Macicior, Daniel Fernandez, Silvia Ortega-Gutierrez
Summary: Hutchinson-Gilford progeria syndrome (HGPS), also known as progeria, is a rare genetic disease that causes premature aging and significantly reduces life expectancy. Currently, there is only one approved drug for treating progeria, but its efficacy is limited. Progerin levels are believed to be the most important biomarker related to disease severity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Fuko Hirano, Naoya Kondo, Yusuke Murata, Aya Sudani, Takashi Temma
Summary: Fluorinated alpha-methyl 3BPA derivatives showed improved water solubility, tumor targetability, and biodistribution compared to 3BPA and BPA, resulting in significantly improved tumor-to-normal tissue ratios.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Ying Shi, Jiaqin Tang, Shumeng Zhi, Ruiqi Jiang, Qing Huang, Lei Sun, Zhizhong Wang, Yanran Wu
Summary: Necroptosis is a type of cell death associated with various diseases. In this study, we identified a small molecule inhibitor, SY-1, that effectively blocks necroptosis by inhibiting the phosphorylation of RIP1/RIP3/MLKL pathway. SY-1 also showed protective effects against TNF-induced hypothermia and improved survival in mice with SIRS. These findings highlight the potential therapeutic applications of SY-1.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Andrea Bagan, Sonia Abas, Judith Pala-Pujadas, Alba Irisarri, Christian Grinan-Ferre, Merce Pallas, Itziar Muneta-Arrate, Carolina Muguruza, Luis F. Callado, Belen Perez, Elies Molins, Jose A. Morales-Garcia, Carmen Escolano
Summary: Recent studies have identified the modulation of imidazoline I-2 receptors (I-2-IR) by selective ligands as a potential strategy for treating neurodegenerative diseases. This study reports a family of bicyclic alpha-iminophosphonates that show high affinity and selectivity for I-2-IR and demonstrates their neuroprotective and anti-inflammatory effects in in vitro and in vivo models. The findings emphasize the importance of exploring structurally novel I-2-IR ligands for therapeutic strategies in neurodegeneration.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Qiuping Xiang, Tianbang Wu, Cheng Zhang, Chao Wang, Hongrui Xu, Qingqing Hu, Jiankang Hu, Guolong Luo, Xiaoxi Zhuang, Xishan Wu, Yan Zhang, Yong Xu
Summary: This study reports the discovery of a 1-(indolizin-3-yl)ethan-1-one derivative as a potent and selective CBP bromodomain inhibitor for AML drug development.
BIOORGANIC CHEMISTRY
(2024)
