Article
Biochemistry & Molecular Biology
Szu Lee, Shih-Wei Wang, Chen-Lin Yu, Huai-Ching Tai, Juei-Yu Yen, Yu-Lien Tuan, Hsueh-Hsiao Wang, Yi-Ting Liu, Shiou-Sheng Chen, Hsueh-Yun Lee
Summary: A series of phenylurea hydroxamic acids containing pharmacophores of HDAC and VEGFR-2 inhibitors were designed, with compound 14 showing antiproliferative activity comparable to Vorinostat and Sorafenib, as well as minimal VEGFR-2 inhibitory activity. Despite its weaker VEGFR-2 activity, compound 14 suggests a potential approach for developing potent HDAC/VEGFR-2 inhibitors.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Bei-Er Jiang, Jiaxin Hu, Hao Liu, Zhitao Liu, Yu Wen, Mingyao Liu, Han-Kun Zhang, Xiufeng Pang, Li-Fang Yu
Summary: In this study, a series of substituted indole-based hydroxamic acid derivatives were designed and synthesized, showing potent antiproliferative activities in various tumor cell lines. Compound 4o was identified as the most potent inhibitor of HDAC1 and HDAC6, exhibiting excellent in vitro anti-tumor proliferation activity and inducing cell cycle arrest and apoptosis. Compound 4o also showed promising results in an HCT116 xenograft mouse model.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Engineering, Chemical
Kuixin Cui, Nan Duan, Shengming Jin
Summary: This study investigated the flotation behaviors and adsorption of 2-(4-Butoxyphenyl)acetohydroxamic acid (BAHA) on rhodochrosite, calcite, and dolomite. The results showed that rhodochrosite had better floatability and higher BAHA adsorption compared to calcite and dolomite. The interaction mechanisms between BAHA and mineral surfaces were responsible for the differences in the adsorption and floatability of rhodochrosite and gangue minerals.
SEPARATION AND PURIFICATION TECHNOLOGY
(2023)
Article
Chemistry, Medicinal
Yu Bao, Qihao Xu, Lin Wang, Yunfei Wei, Baichun Hu, Jian Wang, Dan Liu, Linxiang Zhao, Yongkui Jing
Summary: Psammaplin A (PsA) is a compound with histone deacetylase (HDAC) inhibition capabilities that acts through the reduced monomer PsA-SH. PsA-SH and 10b induce apoptosis in human leukemia cells and inhibit the growth of several solid tumor cell lines.
ACS MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Organic
Virginija Jakubkiene, Gabrielius Ernis Valiulis, Markus Schweipert, Asta Zubriene, Daumantas Matulis, Franz-Josef Meyer-Almes, Sigitas Tumkevicius
Summary: Histone deacetylases (HDACs) are important in the transcriptional regulation of cells and are potential therapeutic targets for various diseases. This study describes the synthesis of new compounds as potential HDAC inhibitors. The synthesized pyrimidine-based hydroxamic acids showed strong inhibitory activity against HDAC4 and HDAC8, with N-hydroxy-6[6-methy1-2-(methylthio)-5-propylpyrimidin-4-yloxy]hexanamide being the most potent inhibitor.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2022)
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
Biochemistry & Molecular Biology
Isil Nihan Korkmaz, Hasan Ozdemir
Summary: New derivatives of hydroxamic acids were synthesized and their anticancer properties and inhibition effects on enzymes causing multidrug resistance in cancer cells were investigated. The results showed that certain derivatives exhibited significant anticancer effects on lung and cervical cancer cells.
APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Samir Mehndiratta, Mei-Chuan Chen, Yuh-Hsuan Chao, Cheng-Hsin Lee, Jing-Ping Liou, Mei-Jung Lai, Hsueh-Yun Lee
Summary: A series of 3-substituted quinolinehydroxamic acids were synthesized and evaluated for their effects on HDAC6, with two compounds showing potent anti-proliferative activity against human lung cancer and colorectal cancer cells. These compounds displayed remarkable selectivity for HDAC6 and induced DNA double strand fragmentation by activating apoptotic caspase pathway in a concentration dependent manner. Flow cytometric analysis also showed a dose dependent increase of cell population in sub G1 phase.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
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.
Article
Biochemistry & Molecular Biology
Cheng- Lee, Chu-Bin Liao, Chih-Shang Chen, Fen-Ying Cheng, Yu-Hsuan Chung, Yu-Chuan Wang, Sian-Yi Ciou, Wen-Yun Hsueh, Tzu-Hao Lo, Guan-Ru Huang, Hsin-Yi Huang, Chia-Shen Tsai, Yu-Jung Lu, Shih-Hsien Chuang, Jiann-Jyh Huang
Summary: This paper describes the design and synthesis of 4-(3-hydroxyanilino)-6-(1H-1,2,3-triazol-4-yl)quinazoline derivative 9 as selective B-Raf/B-RafV600E and potent EGFR/VEGFR2 kinase inhibitors. Among the compounds synthesized, 9m showed the most potent inhibitory activity, selectively targeting B-Raf and B-RafV600E. However, despite its high activity in enzymatic assays, 9m exhibited inferior efficacy in inhibiting melanoma A375 cells.
BIOORGANIC CHEMISTRY
(2021)
Review
Chemistry, Inorganic & Nuclear
Md Lutfor Rahman, Mohd Sani Sarjadi, Shaheen M. Sarkar, Daniel J. Walsh, John J. Hannan
Summary: Functional residues of hydroxamic acid allow it to form complexes with a wide range of metals, contributing to its potential applications in antifungal and anticancer drug development. Poly(hydroxamic acid) possesses similar coordination functionality as the monomeric form, showing diverse potential uses.
COORDINATION CHEMISTRY REVIEWS
(2022)
Article
Engineering, Chemical
Zhihao Guo, Sultan Ahmed Khoso, Jinggang Wang, Chenyang Zhang, Zhiyong Gao, Wei Sun, Mengjie Tian, Yuling Liu
Summary: This manuscript investigates the performance and interaction mechanism of 2-hydroxy-3-naphthyl hydmxamic acid (2-OH-3-NHA) and 1-hydroxy-2-naphthyl hydmxamic acid (1-OH-2-NHA) as flotation collectors for the separation of bastnaesite/fluorite. The results show the excellent selectivities of NHAs and the better selectivity of 1-OH-2-NHA than 2-OH-3-NHA. Zeta potential measurements and first-principles calculations provide insights into the adsorption behavior and selectivity.
SEPARATION AND PURIFICATION TECHNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Chuansheng Yao, Xiaoying Jiang, Rui Zhao, Zhichao Zhong, Jiamin Ge, Junlong Zhu, Xiang-Yang Ye, Yuanyuan Xie, Zhen Liu, Tian Xie, Renren Bai
Summary: A series of dual inhibitors targeting HDAC1/MAO-B were synthesized and found to be promising agents for the treatment of Alzheimer's disease, exhibiting good activity, selectivity, antioxidant activity, and blood-brain barrier penetration. Hybrid If showed the most potent activity and selectivity against MAO-B and HDAC1, as well as favorable antioxidant activity.
BIOORGANIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Meng Li, Na Xue, Xingang Liu, Qiaoyun Wang, Hongyi Yan, Yifan Liu, Lei Wang, Xiaowei Shi, Deying Cao, Kai Zhang, Yang Zhang
Summary: The study designed and synthesized a series of compounds using the classical pharmacophore fusion strategy, which showed promising anti-proliferative activity and low enzyme inhibition levels. Compound 7i displayed excellent antitumor activity and enhanced binding affinity to EGFR by extending into the effective region and interacting with specific residues. This research provides valuable insights for the development of antitumor agents based on EGFR inhibitors.
FRONTIERS IN PHARMACOLOGY
(2021)
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
Plant Sciences
Dinghong Li, Zhao Lei, Jiayu Xue, Guangcan Zhou, Yueyu Hang, Xiaoqin Sun
Article
Genetics & Heredity
Lan-Hua Qian, Guang-Can Zhou, Xiao-Qin Sun, Zhao Lei, Yan-Mei Zhang, Jia-Yu Xue, Yue-Yu Hang
G3-GENES GENOMES GENETICS
(2017)
Article
Plant Sciences
Shanshan Dong, Jia-Yu Xue, Shouzhou Zhang, Li Zhang, Hong Wu, Zhiduan Chen, Bernard Goffinet, Yang Liu
Editorial Material
Plant Sciences
Zhu-Qing Shao, Jia-Yu Xue, Qiang Wang, Bin Wang, Jian-Qun Chen
TRENDS IN PLANT SCIENCE
(2019)
Article
Plant Sciences
Jia-Yu Xue, Yue Wang, Min Chen, Shanshan Dong, Zhu-Qing Shao, Yang Liu
FRONTIERS IN PLANT SCIENCE
(2020)
Editorial Material
Genetics & Heredity
Jia-Yu Xue, Frank L. W. Takken, Madhav P. Nepal, Takaki Maekawa, Zhu-Qing Shao
FRONTIERS IN GENETICS
(2020)
Article
Plant Sciences
Jia-Yu Xue, Shan-Shan Dong, Ming-Qiang Wang, Tian-Qiang Song, Guang-Can Zhou, Zhen Li, Yves Van de Peer, Zhu-Qing Shao, Wei Wang, Min Chen, Yan-Mei Zhang, Xiao-Qin Sun, Hong-Feng Chen, Yong-Xia Zhang, Shou-Zhou Zhang, Fei Chen, Liang-Sheng Zhang, Cymon Cox, Yang Liu, Qiang Wang, Yue-Yu Hang
Summary: The early diversification of angiosperms was a rapid process, leading to conflicting hypotheses regarding overall angiosperm phylogeny. Studies of mitochondrial genomes filled taxon-sampling gaps in various angiosperm lineages and provided additional evidence for exploring the early evolution and diversification of angiosperms. Despite conflicting phylogenies, there was congruence regarding deep relationships of several major angiosperm lineages, with third codon positions of mitochondrial genes producing better resolved phylogenetic relationships.
JOURNAL OF SYSTEMATICS AND EVOLUTION
(2022)
Article
Genetics & Heredity
Jia Liu, Suobing Zhang, Pengfei Xie, Long Wang, Jia-Yu Xue, Yanmei Zhang, Ruisen Lu, Yueyu Hang, Yue Wang, Xiaoqin Sun
Summary: This study evaluated the fitness effects of the susceptible allele of the R gene Pi-ta in rice crops. The loss-of-function of the susceptible allele resulted in significant declines in grain yield. The susceptible allele may serve as a regulator of plant defense responses by turning off downstream immune signaling. This study suggests that susceptible alleles of R genes may have pleiotropic functions and can be maintained in populations.
Article
Plant Sciences
Jia-Yu Xue, Zhen Li, Shuai-Ya Hu, Shu-Min Kao, Tao Zhao, Jie-Yu Wang, Yue Wang, Min Chen, Yichun Qiu, Hai-Yun Fan, Yang Liu, Zhu-Qing Shao, Yves Van de Peer
Summary: Saururus chinensis is an herbaceous magnoliid that attracts insect pollinators through its white leaves during flowering. By studying its genome, we found the phylogenetic position of S. chinensis and identified candidate genes involved in leaf formation. Despite being herbaceous, S. chinensis still has the potential for woody growth due to preserved genes involved in lignin biosynthesis. Overall, the genome of S. chinensis provides insights into the adaptive evolution of pollination and the evolution of herbaceousness in magnoliids.
Article
Genetics & Heredity
Wen Li, Xin-Cheng Huang, Yi-Lei Wang, Rui-Ju Zhang, Dong-Yan Shi, Teng-Fei Li, Guang-Can Zhou, Jia-Yu Xue
Summary: In this study, plastid genome sequencing was performed on 10 representative tree peony cultivars. Comparative analysis of the genomes revealed differences in structure among the cultivars. Phylogenetic relationships between the cultivars and the evolutionary trajectory of flower architecture in the Paeoniaceae family were also investigated.
Article
Genetics & Heredity
Ying Xu, Jia-Yi Wu, Qing-Jie Liu, Jia-Yu Xue
Summary: By studying the genomes of 999 Bacillus species, including 47 different species, it was found that three critical genes (SrfAA, SrfAB, and SrfAC) could be divided into 66 orthologous gene groups. These genes showed high sequence similarity and were not grouped monophyletically, but rather scattered. The study suggests that self-duplication and tandem duplication might have played a role in the initial establishment of the SrfA operon, while gene fusion, recombination, and accumulated mutations continuously shaped the different functional roles of SrfAA, SrfAB, and SrfAC. This research provides new insights into metabolic gene clusters and operon evolution in bacteria.
Article
Plant Sciences
Jia-Yu Xue, Hai-Yun Fan, Zhen Zeng, Yu-Han Zhou, Shuai-Ya Hu, Sai-Xi Li, Ying-Juan Cheng, Xiang-Ru Meng, Fei Chen, Zhu-Qing Shao, Yves Van de Peer
Summary: MicroTom is a prospective model plant for studying organ development, metabolism, and plant-microbe interactions. By constructing gene co-expression networks and non-coding RNA networks, valuable clues for important genes involved in diverse regulatory pathways during plant growth can be identified. The established database provides valuable information for researchers studying organ differentiation and development.
HORTICULTURE RESEARCH
(2023)
Editorial Material
Horticulture
Yufan Liang, Fei Chen, Jia-Yu Xue
Article
Plant Sciences
Jian Zhang, Xin-Xing Fu, Rui-Qi Li, Xiang Zhao, Yang Liu, Ming-He Li, Arthur Zwaenepoel, Hong Ma, Bernard Goffinet, Yan-Long Guan, Jia-Yu Xue, Yi-Ying Liao, Qing-Feng Wang, Qing-Hua Wang, Jie-Yu Wang, Guo Qiang Zhang, Zhi-Wen Wang, Yu Jia, Mei-Zhi Wang, Shan-Shan Dong, Jian-Fen Yang, Yuan-Nian Jiao, Ya-Long Guo, Hong-Zhi Kong, An-Ming Lu, Huan-Ming Yang, Shou-Zhou Zhang, Yves Van de Peer, Zhong-Jian Liu, Zhi-Duan Chen
Article
Genetics & Heredity
Jia-Yu Xue, Tao Zhao, Yang Liu, Yong-Xia Zhang, Guo-Qiang Zhang, Hongfeng Chen, Guang-Can Zhou, Shou-Zhou Zhang, Zhu-Qing Shao
FRONTIERS IN GENETICS
(2020)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
