Article
Immunology
Martina Mazzocchi, Susan R. Goulding, Noelia Morales-Prieto, Tara Foley, Louise M. Collins, Aideen M. Sullivan, Gerard W. O'Keeffe
Summary: The peripheral administration of Class IIa-specific HDIs may have neuroprotective effects in Parkinson's disease.
BRAIN BEHAVIOR AND IMMUNITY
(2022)
Article
Microbiology
Juanbin Yin, Shasha Wang, Shanhui Ren, Zhengji Liang, Junwei Ge, Yuefeng Sun, Xiangping Yin, Xiangwei Wang
Summary: TMP269, a small molecular inhibitor of IIa histone deacetylase, has been found to play a vital role in cancer therapeutic. This study discovered that TMP269 treatment can significantly inhibit the replication of RABV virus without significant cytotoxicity. It was also found that TMP269 can reduce viral titers and protein levels of RABV at an early stage in the viral life cycle. RNA sequencing data revealed that immune-related pathways and autophagy-related genes were downregulated after RABV infection treated with TMP269. Further exploration showed that autophagy enhances RABV replication, while TMP269 can inhibit autophagy to decrease RABV replication. These findings provide a novel treatment strategy for rabies.
FRONTIERS IN MICROBIOLOGY
(2023)
Article
Reproductive Biology
Satoshi Kamimura, Kimiko Inoue, Eiji Mizutani, Jin-Moon Kim, Hiroki Inoue, Narumi Ogonuki, Kei Miyamoto, Shunya Ihashi, Nobuhiko Itami, Teruhiko Wakayama, Akihiro Ito, Norikazu Nishino, Minoru Yoshida, Atsuo Ogura
Summary: The study found that using chlamydocin analogues, which specifically inhibit I and IIa class HDACs, can improve the efficiency of mouse SCNT, with Ky-9 showing similar results to trichostatin A. The one-cell stage was identified as a critical period for enhancing cloning through the use of HDAC inhibitors in SCNT.
BIOLOGY OF REPRODUCTION
(2021)
Review
Biochemistry & Molecular Biology
Ligong Liu, Lilong Dong, Erika Bourguet, David P. Fairlie
Summary: This review summarizes the phenotypes of individual class IIa HDAC proteins and compounds targeting their enzymatic catalytic domain, focusing on their effects in gene regulation and disease. Silencing selected class IIa HDACs or their enzymatic properties can have beneficial or detrimental effects. Targeting the CD of class IIa HDACs may lead to more selective therapeutic agents with fewer side-effects.
CURRENT MEDICINAL CHEMISTRY
(2021)
Review
Cell Biology
Saikat Dewanjee, Jayalakshmi Vallamkondu, Rajkumar Singh Kalra, Pratik Chakraborty, Moumita Gangopadhyay, Ranabir Sahu, Vijaykrishna Medala, Albin John, P. Hemachandra Reddy, Vincenzo De Feo, Ramesh Kandimalla
Summary: Diabetes mellitus is a major manifestation of metabolic syndrome with increasing prevalence. Chronic hyperglycemia can lead to various vascular complications, being the major cause of morbidity and mortality in diabetic patients. Histone deacetylase (HDAC) plays a crucial role in regulating molecular activities in diabetes and could serve as a potential therapeutic target for developing novel intervention strategies.
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
Yi-An Chen, Cheng-Hsiu Lu, Chien-Chih Ke, Sain-Jhih Chiu, Chi-Wei Chang, Bang-Hung Yang, Jun G. Gelovani, Ren-Shyan Liu
Summary: The study revealed an association between class IIa HDACs and A beta, therapeutic benefits of a selective HDAC4 inhibitor, and the potential of using [F-18]TFAHA as an epigenetic radiotracer for AD, which could aid in the development of AD-related neuroimaging approaches and therapies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Christian Schrenk, Lukas M. Bollmann, Corinna Haist, Arthur Bister, Constanze Wiek, Maria Wecker, Dennis Roth, Patrick Petzsch, Karl Koehrer, Alexandra Hamacher, Helmut Hanenberg, Georg Fluegen, Matthias U. Kassack
Summary: In contrast to class I/IIb/pan histone deacetylase inhibitors (HDACi), the role of class IIa HDACi as anti-cancer chemosensitizing agents is less well understood. Here, we studied the effects of HDAC4 in particular and the class IIa HDACi CHDI0039 on proliferation and chemosensitivity in Cal27 and cisplatin-resistant Cal27CisR head and neck squamous cell cancer (HNSCC). The combination of class IIa HDACi with proteasome inhibitors constitutes an effective treatment option for HNSCC, particularly for platinum-resistant cancers.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Lukas M. Bollmann, Alexander J. Skerhut, Yodita Asfaha, Nadine Horstick, Helmut Hanenberg, Alexandra Hamacher, Thomas Kurz, Matthias U. Kassack
Summary: This study introduces a novel highly selective HDAC inhibitor, YAK540, and demonstrates its synergistic cytotoxic effect and proapoptotic effect when combined with the proteasome inhibitor BTZ. The cytotoxicity of the YAK540 and BTZ combination is significantly lower in non-cancer cells compared to leukemia cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Saravanan Kandasamy, Manikandan Selvaraj, Karthikeyan Muthusamy, Naveena Varadaraju, Srinivasan Kannupal, Ashok Kumar Sekar, Ravikumar Vilwanathan
Summary: HDAC inhibitors are a new class of cancer chemotherapeutics that restore acetylation balance and inhibit HDAC enzymes. Berberine is a pan inhibitor for HDAC, but isoform specific inhibition is still needed. Through structural modification, we obtained berberine derivatives that showed better inhibition of HDAC enzymes and improved clinical efficacy.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Physiology
Zexu Shen, Yun Bei, Haoran Lin, Taofeng Wei, Yunjian Dai, Yangmin Hu, Chao Zhang, Haibin Dai
Summary: Vascular endothelial cells play a crucial role in maintaining homeostasis and are regulated by signaling pathways and epigenetic factors. Dysfunctions in endothelial cells are associated with cardiovascular and cerebrovascular diseases. Histone deacetylases (HDACs), especially Class IIa HDACs, have limited activity and tissue-specific regulation in endothelial cells. In this article, we discuss the functions of HDACs in endothelial cells, including angiogenesis and immune response, and propose potential applications of HDAC inhibitors for the treatment of vascular diseases.
FRONTIERS IN PHYSIOLOGY
(2023)
Article
Chemistry, Medicinal
Dimitrios Triantafyllos Gerokonstantis, Christiana Mantzourani, Dimitrios Gkikas, Kai-Chen Wu, Huy N. Hoang, Ierasia Triandafillidi, Ilianna Barbayianni, Paraskevi Kanellopoulou, Alexandros C. Kokotos, Panagiota Moutevelis-Minakakis, Vassilis Aidinis, Panagiotis K. Politis, David P. Fairlie, George Kokotos
Summary: Benzamides, as HDAC inhibitors, have shown promising anticancer activity and potential for treating fibrotic disorders.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Engineering, Environmental
Jue Ling, Yi Luo, Cheng Sun, Zhangji Dong, Ronghua Wu, Xiaoxuan Tang, Nan Du, Rui Zhu, Shi Chen, Mei Liu, Yan Liu, Yongjun Wang, Xiaosong Gu, Yong Ling, Yumin Yang
Summary: This study introduces an intraoperative therapeutic strategy using a multifunctional fluorescent probe for highly sensitive and selective real-time diagnosis of micrometastases in zebrafish and mice, and significant tumor inhibition against colon cancer and hepatic metastasis.
CHEMICAL ENGINEERING JOURNAL
(2021)
Article
Chemistry, Medicinal
Xingrui He, Zi Hui, Li Xu, Renren Bai, Yuan Gao, Zongcheng Wang, Tian Xie, Xiang-Yang Ye
Summary: Histone deacetylases (HDACs) are important enzymes involved in the removal of acetyl groups from lysine residues, and have shown potential therapeutic applications in cancer and various diseases. There are currently numerous HDAC inhibitors under clinical investigation, aiming to provide up-to-date information for drug discovery programs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(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, Physical
Jiabao Li, Ziqian Li, Shaocong Tang, Jingjing Hao, Tianyi Wang, Chengyin Wang, Likun Pan
Summary: A systematic study on the sodium storage performance of carbonaceous anodes derived from bimetallic-organic frameworks was conducted. By adjusting the inner structure from hierarchical disordered structure to gradually increased graphitic ordered domains, an optimized structure with rich micropores/mesopores and ordered domains was obtained, exhibiting excellent sodium storage performances.
Article
Energy & Fuels
Xiaoyu Zhou, Hang Liu, Sixiao Liu, Lei Zhang, Tianyi Wang, Chengyin Wang, Dawei Su
Summary: By using the α-Fe2O3/g-C3N4/HNTs composite material, efficient photocatalytic desulfurization of dibenzothiophene in model oil under visible light can be achieved. The unique structure of the composite material promotes the transfer and separation of photogenerated carriers, thereby enhancing the efficiency of photocatalytic reactions.
Article
Chemistry, Physical
Jiabao Li, Ziqian Li, Shaocong Tang, Tianyi Wang, Kai Wang, Likun Pan, Chengyin Wang
Summary: This study presents a novel hybrid structure consisting of sodium titanium phosphate (NTP) nanocube decorated on carbon, demonstrating excellent sodium storage performances at low temperatures. The hybrid structure, with its superionic conductor structure, flat voltage plateaus, and conductive carbonaceous framework, facilitates charge transfer, accelerates Na' diffusion, and reduces electrochemical polarization.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2023)
Article
Chemistry, Physical
Jiabao Li, Shaocong Tang, Ziqian Li, Zibiao Ding, Tianyi Wang, Chengyin Wang
Summary: Researchers have developed a three-dimensional cross-linked heterostructure with one-dimensional amorphous potassium titanate nanobelts grown on two-dimensional titanium carbide nanosheets, which improves the low-temperature performance of sodium-ion batteries.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Yanyan Zhang, Yue Xi, Changshui Yang, Weijuan Gong, Chengyin Wang, Liang Wu, Dongxu Wang
Summary: This study investigated the anti-inflammatory effects of short-chain fatty acids (SCFAs), including sodium acetate, sodium propionate, and sodium butyrate, on 5-fluorouracil (5-FU)-induced macrophage inflammation. The results showed that the three SCFAs inhibited pro-inflammatory factor expressions and ROS/NF-kappa B/NLRP3 signaling pathway. They also regulated glycerophospholipid and sphingolipid metabolism. This is the first identification of SCFAs as inhibitors of 5-FU-induced macrophage inflammation.
Article
Biochemistry & Molecular Biology
Luisa M. Bachmann, Maria Hanl, Felix Feller, Laura Sinatra, Andrea Schoeler, Jens Pietzsch, Markus Laube, Finn K. Hansen
Summary: Multi-target drugs (MTDs) offer a new approach for combination therapies. In this study, a library of dual HDAC-COX inhibitors was designed, synthesized, and evaluated. The synthesized compounds showed significant inhibitory activities against HDAC and COX isoforms. Selected compounds were confirmed to have membrane permeability and inhibition of cellular HDAC activity. The most promising dual inhibitors, C3 and C4, demonstrated antiproliferative effects and increased apoptotic cells. However, simultaneous inhibition of HDAC and COX by these inhibitors or combination treatments did not result in additive or synergistic anticancer activities.
Article
Chemistry, Physical
Yu Wang, Jiabao Li, Penghao Song, Jian Yang, Zhihao Gu, Tianyi Wang, Chengyin Wang
Summary: In this study, a three-dimensional interconnected SnS/Nb2CTx composite material was fabricated through a facile solvothermal approach, which exhibited excellent electronic conductivity and fast charge-discharge kinetics. The SnS/Nb2CTx system demonstrated superior electrochemical performance due to its excellent electronic/ionic conductivity, efficient buffering matrix, abundant active sites, and high sodium storage activity, with reversible capacities of 479.6 mAh/g (0.1 A/g, 100 cycles) and 278.9 mAh/g (0.5 A/g, 500 cycles) upon sodium storage, respectively.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2023)
Article
Chemistry, Physical
Jian Yang, Xin Guo, Hong Gao, Tianyi Wang, Zhigang Liu, Qing Yang, Hang Yao, Jiabao Li, Chengyin Wang, Guoxiu Wang
Summary: This study reports a surface and interface engineering strategy to improve the electrochemical performance of sodium-ion batteries by surface engineering of tin nanorods via N-doped carbon layers (Sn@NC). The authors demonstrate that uniform surface modification can enhance electron and sodium transport kinetics, control alloy pulverization, and form a stable organic-inorganic solid-electrolyte interface (SEI). It is also discovered that the diethylene glycol dimethyl ether electrolyte with optimized Na+ solvation structure can significantly improve reaction kinetics. Consequently, Sn@NC anodes achieve extra-long cycling stability and the full cell exhibits high energy density, excellent high-rate capability, and long cycle life over a wide temperature range.
ADVANCED ENERGY MATERIALS
(2023)
Article
Nanoscience & Nanotechnology
Penghao Song, Jian Yang, Chengyin Wang, Tianyi Wang, Hong Gao, Guoxiu Wang, Jiabao Li
Summary: Heterostructure engineering combined with carbonaceous materials has shown great promise for improving the performance of transition metal sulfide electrodes in high-performance sodium storage. A specific iron sulfide-based heterostructure (Fe7S8/FeS2/NCNT) with nitrogen-doped carbon nanotubes has been prepared, which demonstrated high reversible capacity, superior rate capability, long-term cycling stability, and outstanding rate capability in different electrolytes. The outstanding performance is mainly attributed to fast sodium-ion diffusion kinetics, high capacitive contribution, and convenient interfacial dynamics.
NANO-MICRO LETTERS
(2023)
Article
Oncology
Emil Novruzov, Dominik Schmitt, Katalin Mattes-Gyoergy, Markus Beu, Yuriko Mori, Mardjan Dabir, Jan Philipp Radtke, Guenter Niegisch, Peter Albers, Lars Schimmoeller, Gerald Antoch, Christina Antke, Frederik L. Giesel, Eduards Mamlins
Summary: Through a study on 19 male patients with prostate cancer, it was found that there is a higher detection rate of ganglia in imaging with [18F]PSMA-1007 compared to [68Ga]Ga-PSMA-11. The study also suggests that the better detectability is not due to higher uptake but rather more favorable physical properties of [F-18]PSMA-1007.
Article
Oncology
Karim Fizazi, Neal D. Shore, Matthew Smith, Rodrigo Ramos, Robert Jones, Guenter Niegisch, Egils Vjaters, Yuan Wang, Shankar Srinivasan, Toni Sarapohja, Frank Verholen
Summary: Darolutamide significantly improved the survival rate of nmCRPC patients and showed a favorable safety profile during the treatment.
EUROPEAN JOURNAL OF CANCER
(2023)
Article
Chemistry, Physical
Jian Yang, Jiabao Li, Jiahui Lu, Xiaoxue Sheng, Yu Liu, Tianyi Wang, Chengyin Wang
Summary: In this study, a unique structure of antimony selenide nanowires uniformly anchored between MXene nanosheets was prepared, which overcame the issues of volume expansion, sluggish kinetics, and polyselenide shuttle of the antimony selenide anode, resulting in high rate capability and cycling performance.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2023)
Article
Materials Science, Multidisciplinary
Jiabao Li, Ziqian Li, Shaocong Tang, Tianyi Wang, Likun Pan, Chengyin Wang
Summary: The NVP cathode (F-NVP/C@3DNC) with F substitution and V vacancies as well as 3D nitrogen-doped carbonaceous frameworks showed improved electronic conductivity and ion conductivity, leading to high specific capacity and capacity retention even at low temperatures.
JOURNAL OF MATERIALS SCIENCE & TECHNOLOGY
(2023)
Article
Chemistry, Medicinal
Beate Ko''nig, Paris R. Watson, Nina Ressing, Abigail D. Cragin, Linda Scha''ker-Hu''bner, David W. Christianson, Finn K. Hansen
Summary: Histone deacetylase 6 (HDAC6) is a significant target for drug development in both oncological and non-oncological diseases. Recent findings suggest that difluoromethyl-1,3,4-oxadiazoles (DFMOs) can act as potent and selective HDAC6 inhibitors, but the mechanism of inhibition has not been well understood. This study reveals that DFMOs function as mechanism-based and essentially irreversible HDAC6 inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Max E. E. Huber, Silas Wurnig, Lara Toy, Corinna Weiler, Nicole Merten, Evi Kostenis, Finn K. K. Hansen, Matthias Schiedel
Summary: In this study, a fluorescent ligand targeting the intracellular allosteric binding site (IABS) of CXCR2 was developed. The ligand, Mz438 (9a), exhibited high affinity and selectivity and could be used for visualizing intracellular target engagement. This fluorescent ligand represents a promising tool for future studies of CXCR2 pharmacology.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)