Article
Chemistry, Medicinal
Qingling Chen, Zhuoying Chen, Feilong Li, Haoyu Zha, Wei He, Fei Jiang, Jiamu Wei, Jiajia Xu, Rong Li, Li Cai, Xuesong Liu
Summary: This study identified indazole derivatives as a novel class of potent VEGFR2 inhibitors, with compound 25 being the most effective. Compound 25 exhibited good selectivity for VEGFR2 and inhibited VEGFR2 phosphorylation and angiogenesis in HUVECs. It also showed anti-arthritic and anti-angiogenic effects in rats.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Immunology
Ning Zhang, Changqing Zhang, Zhihong Zeng, Jiyong Zhang, Shengnan Du, Chunde Bao, Zhe Wang
Summary: The study introduced a novel JAK1-specific inhibitor LW402, demonstrating potent efficacy in rat and mouse arthritis models and establishing good safety profile in toxicity studies. LW402 exhibits a high therapeutic window, indicating promising clinical applications.
JOURNAL OF INFLAMMATION RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Tingting Liang, Lifang Cen, Junjie Wang, Ming Cheng, Weibo Guo, Wenjie Wang, Chunqiu Yu, Haifeng Zhang, Yuan Wang, Zhongyan Hao, Jiaming Jin, Yaoyao Wu, Teng Jiang, Qihua Zhu, Yungen Xu
Summary: The discovery of the dual BTK/JAK3 inhibitor compound XL-12 has shown potent anti-rheumatoid arthritis activity both in vitro and in vivo, with improved safety compared to ibrutinib.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Abdelmoujoud Faris, Hanine Hadni, Ibrahim M. Ibrahim, Menana Elhallaoui
Summary: In this study, a comprehensive theoretical approach was employed to propose and optimize new anti-JAK3 compounds for the treatment of rheumatoid arthritis. A highly accurate 3D-QSAR model was developed using COMSIA, and covalent docking studies identified highly potent JAK3 inhibitors. ADMET properties and drug similarity were evaluated, and molecular dynamics simulations confirmed the stability of the designed compounds.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Medicinal
Shan Li, Hongfei Si, Xiaojuan Song, Chong Lei, Xiaoqiang He, Jie Wang, Yiling Liu, Yang Zhou, Jian-Guo Song, Lijie Peng, Xia Tang, Shingpan Chan, Xiaomei Ren, Zhengchao Tu, Zhengqiu Li, Zhen Wang, Zhang Zhang, Ke Ding
Summary: The discovery of a series of new orally bioavailable irreversible JAK3 kinase inhibitors, with compound 12n as a promising lead compound for the treatment of hematological malignancies.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Chao Yang, Yuan Fang, Xiang Luo, Dehong Teng, Zhongqiu Liu, Yingtang Zhou, Guochao Liao
Summary: FY-56 is a highly potent and selective LSD1 inhibitor that can inhibit the proliferation of leukemia cells and induce differentiation, showing therapeutic potential for AML treatment.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Xiaobao Fang, Chunxiao Liu, Kun Zhang, Wanping Yang, Zewen Wu, Shige Shen, Yule Ma, Xun Lu, Yadong Chen, Tao Lu, Qinghua Hu, Yulei Jiang
Summary: This study discovered a series of novel, potent, and selective covalent BTK inhibitors through structure-based drug design, among which compound 36R exhibited high kinase selectivity, long target occupancy time, appropriate pharmacokinetic properties, and dose-dependent efficacy in a rat model of collagen-induced arthritis. Therefore, 36R is a novel BTK inhibitor requiring further development for the treatment of autoimmune diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Agriculture, Multidisciplinary
Yu-Meng Zhang, Jian Shen, Jun-Ming Zhao, Jian Guan, Xin-Rui Wei, Dong-Yu Miao, Wei Li, Yi-Cheng Xie, Yu-Qing Zhao
Summary: Cedrol (CE) derived from ginger demonstrates efficacy in ameliorating rheumatoid arthritis through anti-inflammatory and immunological enhancement effects. The mechanism of CE involves inhibition of JAK3 protein phosphorylation, leading to reduced secretion of pro-inflammatory cytokines and inflammation mediators. Pharmacokinetic results show varying absolute bioavailability of CE at different dosages, indicating its potential for further application.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Nuria Bielsa, Mireia Casasampere, Mazen Aseeri, Josefina Casas, Antonio Delgado, Jose Luis Abad, Gemma Fabrias
Summary: This study identifies highly selective ACER3 activity blockers in intact cells, paving the way for further medicinal chemistry efforts aimed at developing more potent and specific compounds.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Scott Scarneo, Philip Hughes, Robert Freeze, Kelly Yang, Juliane Totzke, Timothy Haystead
Summary: Selective targeting of TNF has provided therapeutic benefit in inflammatory diseases like rheumatoid arthritis, but the development of antidrug antibodies limits long-term efficacy, necessitating the development of alternative treatments. Targeting the protein kinase TAKI has shown promise in providing an effective alternative to frontline biologic-based RA therapeutics.
ACS CHEMICAL BIOLOGY
(2022)
Article
Biology
Izzuddin Ahmad Nadzirin, Adam Leow Thean Chor, Abu Bakar Salleh, Mohd Basyaruddin Abdul Rahman, Bimo A. Tejo
Summary: Rheumatoid arthritis is an inflammatory autoimmune disease affecting about 0.24% of the world population, and PAD4 is believed to be responsible for its occurrence. Peptide inhibitors designed to target PAD4 can reduce its activity, with P2 (Cav) showing potential as an inhibitor against PAD4 based on experimental data.
COMPUTATIONAL BIOLOGY AND CHEMISTRY
(2021)
Article
Chemistry, Analytical
Xin-Fang Zhai, Yang Yi, Rong Yu, Yi Kuang, Sharpkate Shaker, Hui-Fei Su, Guo Ye, Chen-Rui Liu, Xue Qiao, Lei Liang, Min Ye
Summary: In this study, we developed a novel fluorescent probe, NHPF, that exhibits excellent selectivity and sensitivity towards UGT1A1. NHPF was utilized for real-time imaging of endogenous UGT1A1 in living cells and identification of UGT1A1 inhibitors and activators from licorice, a traditional Chinese medicine.
SENSORS AND ACTUATORS B-CHEMICAL
(2022)
Article
Biochemistry & Molecular Biology
Kazuo Shimizu, Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Kazuya Tatani, Kenji Katsuno, Yoshikazu Fujimori, Shinjiro Watanabe, Masahiro Hiratochi, Takeshi Nakabayashi, Noboru Kamada, Koichi Arakawa, Hidemasa Hikawa, Isao Azumaya, Masayuki Isaji
Summary: By optimizing the structure, O-glucoside derivative 24 (remogliflozin etabonate) was identified as a potent, highly selective, and orally available SGLT2 inhibitor.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Zhengyu Fang, Yiping Hu, Jiajing Dai, Lianhua He, Juan He, Bihua Xu, Xinle Han, Fubo Zhong, Huiyao Lan, Qingwen Wang
Summary: The combination treatment with CS12192 and MTX is shown to have a better therapeutic effect on collagen-induced arthritis (CIA) in rats, with a stronger suppressive effect on T cells and macrophage-mediated joint inflammation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Vijay Kanoje, Dilip Pandey, Akshaya Wagh, Sukanya Patra, Ajit Kumar Marisetti, Madhusudhan Reddy, Charudatt Samant, Nilesh Mahajan, Milind Gholve, Sudeep Sabde, Sneha Trivedi, Trupti Bhankhede, Vinod Patil, Prashant Nigade, Dipak Modi, Maneesh Mehta, Prajakta Ahirrao, Swathi Tota, Bidyut Nanda, Shashikant Pawar, Anuradha Polawar, Kaustubh Tamane, Sandip Kuldharan, Gururaj Vishwase, Nirmal Jana, Sachin J. Mahangare, Prashant Vidhate, Dipak Lagad, Jayasagar Gundu, Samiron Phukan, Manojkumar Shukla, Lakshmi Narasimham, Kumar V. S. Nemmani, Mandar Bhonde, Sharad Sharma, Rajender K. Kamboj, Venkata P. Palle
Summary: This study describes the in vitro and in vivo activity and drug-like properties of the PI3K delta specific inhibitor LL-00071210 in rheumatoid arthritis models. LL-00071210 shows excellent selectivity and stability, demonstrating potential as a clinical drug for the treatment of autoimmune diseases.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Oncology
Qiheng Gou, Linbo Gao, Xinwen Nie, Wenchen Pu, Jingqiang Zhu, Yichao Wang, Xuesha Liu, Shuangyan Tan, Jian-Kang Zhou, Yanqiu Gong, Juan He, Ke Wu, Yuxin Xie, Wanjun Zhao, Lunzhi Dai, Lunxu Liu, Rong Xiang, Yu-Quan Wei, Lin Zhang, Yong Peng
Article
Medicine, Research & Experimental
Yanqiu Gong, Wenchen Pu, Hongyu Jin, Pei Yang, Hao Zeng, Yuqi Wang, Fuwen Pang, Xuelei Ma
Article
Cell Biology
Qijie Li, Liangbin Lin, Yanli Tong, Yantong Liu, Jun Mou, Xiaodong Wang, Xiuxuan Wang, Yanqiu Gong, Yi Zhao, Yi Liu, Bo Zhong, Lunzhi Dai, Yu-Quan We, Huiyuan Zhang, Hongbo Hu
Article
Biochemical Research Methods
Yu Liu, Zhigui Li, Zhiqiang Xu, Xiuxiu Jin, Yanqiu Gong, Xuyang Xia, Yuqin Yao, Zhaofen Xu, Yong Zhou, Heng Xu, Shuangqing Li, Yong Peng, Xiaoting Wu, Lunzhi Dai
MOLECULAR & CELLULAR PROTEOMICS
(2019)
Article
Gastroenterology & Hepatology
Zhao Huang, Jian-Kang Zhou, Kui Wang, Haining Chen, Siyuan Qin, Jiayang Liu, Maochao Luo, Yan Chen, Jingwen Jiang, Li Zhou, Lei Zhu, Juan He, Jiao Li, Wenchen Pu, Yanqiu Gong, Jianbo Li, Qin Ye, Dandan Dong, Hongbo Hu, Zongguang Zhou, Lunzhi Dai, Canhua Huang, Xiawei Wei, Yong Peng
Article
Biochemistry & Molecular Biology
Xiaofei Shen, Lin Zhao, Peihao Chen, Yanqiu Gong, Dingdong Liu, Xia Zhang, Lunzhi Dai, Qingxiang Sun, Jizhong Lou, Zhong Jin, Baohua Zhang, Dawen Niu, Ceshi Chen, Xiangbing Qi, Da Jia
JOURNAL OF BIOLOGICAL CHEMISTRY
(2019)
Article
Multidisciplinary Sciences
Jingyun Yang, Wei Wang, Zimin Chen, Shuaiyao Lu, Fanli Yang, Zhenfei Bi, Linlin Bao, Fei Mo, Xue Li, Yong Huang, Weiqi Hong, Yun Yang, Yuan Zhao, Fei Ye, Sheng Lin, Wei Deng, Hua Chen, Hong Lei, Ziqi Zhang, Min Luo, Hong Gao, Yue Zheng, Yanqiu Gong, Xiaohua Jiang, Yanfeng Xu, Qi Lv, Dan Li, Manni Wang, Fengdi Li, Shunyi Wang, Guanpeng Wang, Pin Yu, Yajin Qu, Li Yang, Hongxin Deng, Aiping Tong, Jiong Li, Zhenling Wang, Jinliang Yang, Guobo Shen, Zhiwei Zhao, Yuhua Li, Jingwen Luo, Hongqi Liu, Wenhai Yu, Mengli Yang, Jingwen Xu, Junbin Wang, Haiyan Li, Haixuan Wang, Dexuan Kuang, Panpan Lin, Zhengtao Hu, Wei Guo, Wei Cheng, Yanlin He, Xiangrong Song, Chong Chen, Zhihong Xue, Shaohua Yao, Lu Chen, Xuelei Ma, Siyuan Chen, Maling Gou, Weijin Huang, Youchun Wang, Changfa Fan, Zhixin Tian, Ming Shi, Fu-Sheng Wang, Lunzhi Dai, Min Wu, Gen Li, Guangyu Wang, Yong Peng, Zhiyong Qian, Canhua Huang, Johnson Yiu-Nam Lau, Zhenglin Yang, Yuquan Wei, Xiaobo Cen, Xiaozhong Peng, Chuan Qin, Kang Zhang, Guangwen Lu, Xiawei Wei
Article
Cell Biology
Lejiao Mao, Chenyi Liao, Jiao Qin, Yanqiu Gong, Yifei Zhou, Shasha Li, Zhe Liu, Huaqing Deng, Wankun Deng, Qingxiang Sun, Xianming Mo, Yu Xue, Daniel D. Billadeau, Lunzhi Dai, Guohui Li, Da Jia
Summary: This study reveals that external stimuli such as starvation, LPS, and inflammatory cytokines can inhibit endocytic recycling of proteins by activating MAPK11/14, leading to a disruption in the balance between recycling and degradation. Stress-induced kinases phosphorylate SNX27 at Ser51, altering its binding with cargo proteins and thereby suppressing endocytic recycling. The findings suggest that cells can modulate endocytic recycling in response to stress signals, providing new insights into how cells cope with stress and conserve energy.
JOURNAL OF CELL BIOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Li-Qiang Wan, Xia Zhang, Yike Zou, Rong Shi, Jin-Ge Cao, Shi-Yang Xu, Li-Fan Deng, Li Zhou, Yanqiu Gong, Xiaoling Shu, Ga Young Lee, Haiyan Ren, Lunzhi Dai, Shiqian Qi, K. N. Houk, Dawen Niu
Summary: This study presents a nonenzymatic glycosylation reaction that forms axial S-glycosidic bonds under biorelevant conditions. By using allyl glycosyl sulfones as precursors to glycosyl radicals and taking advantage of the exceptional functional group tolerance of radical processes, various unprotected glycosyl units can be selectively introduced to cysteine residues of peptides. The method was successfully applied for direct glycosylation of complex polypeptides and proteins after developing a second-generation protocol, with computational studies performed to elucidate the reaction mechanism.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Biochemistry & Molecular Biology
Yuping Tan, Xia Zhou, Yanqiu Gong, Kun Gou, Youfu Luo, Da Jia, Lunzhi Dai, Yinglan Zhao, Qingxiang Sun
Summary: The study identified a new PHGDH inhibitor, oridonin, and revealed the mechanism of its binding to PHGDH structure, providing new insights for the future design of PHGDH inhibitors.
CELLULAR AND MOLECULAR LIFE SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Yanqiu Gong, Suideng Qin, Lunzhi Dai, Zhixin Tian
Summary: This article reviews the detection, substrates, biological functions of glycosylation in SARS-CoV-2 proteins, as well as the human receptor ACE2. It also summarizes approved and ongoing SARS-CoV-2 therapeutics associated with glycosylation. This review not only helps broaden the understanding of viral glycobiology, but also provides key clues for the development of new preventive and therapeutic methodologies against SARS-CoV-2 and its variants.
SIGNAL TRANSDUCTION AND TARGETED THERAPY
(2021)
Article
Biochemical Research Methods
Yanqiu Gong, Yu Liu, Tian Wang, Zhigui Li, Li Gao, Haining Chen, Yang Shu, Yuan Li, Heng Xu, Zongguang Zhou, Lunzhi Dai
Summary: The occurrence and prevalence of colorectal cancer (CRC) is closely associated with age, with distinct overall survival rates between young and aged patients. However, the underlying mechanisms of age-dependent clinical differences remain elusive.
MOLECULAR & CELLULAR PROTEOMICS
(2021)