Article
Biochemistry & Molecular Biology
Yue Bai, Lu Chen, Pan-Pan Wang, Yu-Qiang Tang, Da-Chang Wu, Cui-Li Zhang, Qi Zhou, Ru Yan, Jie Hou
Summary: The study found that amentoflavone is an effective broad-spectrum inhibitor against bacterial GUS, which can be used as a promising lead compound for developing novel agents to alleviate GUS-associated intestinal toxicity.
Article
Environmental Sciences
Urmi Das, Md Atikur Rahman, Esrat Jahan Ela, Ki-Won Lee, Ahmad Humayan Kabir
Summary: This study demonstrates that supplementation of sulfur can alleviate cadmium toxicity in alfalfa plants by restoring biomass, chlorophyll synthesis, and protein concentration, as well as enhancing photosynthetic kinetics and membrane stability. The mechanisms involve upregulation of sulfate transporters, glutathione and phytochelatin synthesis, and subcellular sequestration of excess cadmium in roots under sulfur surplus conditions. These findings provide valuable insights for developing cadmium-free forage crops through sulfur application and breeding/transgenic experiments.
Article
Chemistry, Medicinal
Lutete Peguy Khonde, Rudolf Mueller, Grant A. Boyle, Virsinha Reddy, Aloysius T. Nchinda, Charles J. Eyermann, Stephen Fienberg, Vinayak Singh, Alissa Myrick, Efrem Abay, Mathew Njoroge, Nina Lawrence, Qin Su, Timothy G. Myers, Helena I. M. Boshoff, Clifton E. Barry, Frederick A. Sirgel, Paul D. van Helden, Lisa M. Massoudi, Gregory T. Robertson, Anne J. Lenaerts, Gregory S. Basarab, Sandeep R. Ghorpade, Kelly Chibale
Summary: A study identified a moderately active compound against Mycobacterium tuberculosis through high-throughput screening, with potential bactericidal activity and retention of activity against drug-resistant strains. Initial investigations suggested inhibition of cell wall biosynthesis as a possible mode of action, but the specific mechanism remains unclear.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Oncology
Lei Wang, Xi Zhu, Lili Li, Lin Li, Li Fu, Yun Li, Haoyu Fu, Xiaoyan Chen, Liguang Lou
Summary: PARP inhibitors have shown promising clinical benefits, but treatment-related toxicities limit their applications. A novel PARP inhibitor, TSL-1502, demonstrated selective inhibitory effects on cancer cells and enhanced chemotherapy sensitivity without causing severe toxicities. TSL-1502 could represent a new potential therapeutic choice for PARP inhibition.
AMERICAN JOURNAL OF CANCER RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Xiang-Ge Tian, Jian-Kun Yan, Cheng-Peng Sun, Jing-Xin Li, Jing Ning, Chao Wang, Xiao-Kui Huo, Wen-Yu Zhao, Zhen-Long Yu, Lei Feng, Xia Lv, Xiao-Chi Ma
Summary: The study revealed the inhibitory effects of Selaginella tamariscina and its major biflavonoid amentoflavone (AMF) on gut bacterial beta-glucuronidase (GUS), indicating their potential clinical utility in treating drug-induced enteropathy. The inhibitory activity of AMF against GUS was demonstrated through IC50 values and inhibition kinetics studies, with molecular docking and dynamics simulation providing insight into the mechanism of action. These findings suggest a promising approach in alleviating drug-induced gastrointestinal toxicity.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Chemistry, Medicinal
Qianqian Qiu, Feng Zou, Huilan Li, Wei Shi, Daoguang Zhou, Ping Zhang, Teng Li, Ziyu Yin, Zilong Cai, Yuxuan Jiang, Wenlong Huang, Hai Qian
Summary: Compound 21 is a dual inhibitor that can block both P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), showing potential in overcoming multidrug resistance and improving the oral bioavailability of specific drugs.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Mahmoud Kandeel, Mizuki Yamamoto, Byoung Kwon Park, Abdulla Al-Taher, Aya Watanabe, Jin Gohda, Yasushi Kawaguchi, Kentaro Oh-hashi, Hyung-Joo Kwon, Jun-ichiro Inoue
Summary: A highly potent set of peptides was designed to prevent MERS-CoV fusion through competition with HR2 at its HR1 binding site. These peptides demonstrated strong inhibition of MERS-CoV cell-cell fusion and plaque formation, with no cytotoxic effects at high concentrations, suggesting their potential as promising antiviral agents.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Muhammad Ikram, Mohammad Naeem, Muhammad Zahoor, Marlia Mohd Hanafiah, Adeleke Abdulrahman Oyekanmi, Noor Ul Islam, Midrar Ullah, Mater H. Mahnashi, Amer Al Ali, Naif A. Jalal, Farkad Bantun, Aiman M. Momenah, Abdul Sadiq
Summary: This study tested several bacterial strains for their ability to degrade the azo dye orange II and found that Bacillus subtilis was the most effective. Optimal conditions for maximum degradation were determined using response surface methodology, and the degradation metabolites were analyzed using various spectroscopic techniques. The results suggest that Bacillus subtilis could be a potential strain for the remediation of textile effluents containing orange II and other toxic azo dyes.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Hiroaki Shimada, Hiroyuki Ikuta, Keisuke Kumazawa, Manato Nomi, Mayumi Shiojiri, Atsushi Kawase, Masahiro Iwaki
Summary: This study evaluated the formation, enzymatic hydrolysis, and chemical instability of acyl glucuronides (AGs) in liver microsomes and their relationship with idiosyncratic drug toxicity (IDT) risk. It was found that enzymatic hydrolysis and chemical instability varied among different drugs, and the rate constant of enzymatic hydrolysis was higher for withdrawn drugs compared to warning and safe drugs.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Chemistry, Medicinal
Ya-Sheng Li, Min He, Tao-Shun Zhou, Qin Wang, Lulu He, Si-Jia Wang, Bei Hu, Bin Wei, Hong Wang, Zi-Ning Cui
Summary: Novel compounds containing 1,3,4-thiadiazole were synthesized and screened for inhibitory activity against enzymes, leading to the discovery of potential inhibitors. Kinetic studies and molecular docking simulations revealed the mechanisms of action of these compounds. Some compounds showed promising therapeutic effects against diseases and side effects.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Guiwei Rao, Hangfei Yu, Manlai Zhang, Yuchen Cheng, Kun Ran, Jianwei Wang, Bin Wei, Min Li, Weiguang Shan, Zhajun Zhan, Youmin Ying
Summary: This study focused on isolating and characterizing AGS and/or BGUS inhibitors from the medicinal plant Schisandra sphaerandra. Eight compounds were identified, with compounds 1-5 showing potent to moderate activity against AGS and compound 3 exhibiting significant BGUS inhibitory activity. These compounds have the potential to be developed as therapeutic agents for Type 2 diabetes mellitus and its complications.
Article
Biochemistry & Molecular Biology
Aditi Vashistha, Nikhil Sharma, Yerramsetti Nanaji, Deepak Kumar, Gurpal Singh, Ravi P. Barnwal, Ashok Kumar Yadav
Summary: The overuse and inappropriate use of antibiotics has led to the development of drug resistant bacterial strains. Biofilm, a complex microorganism aggregation, plays a crucial role in infectious diseases. Efforts to disrupt biofilms have identified molecules that can inhibit quorum sensing, offering potential treatments for bacterial infections with lower dosages of medications.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yang Zheng, Magali van den Kerkhof, Tiffany van der Meer, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Iwan J. P. de Esch, Marco Siderius, An Matheeussen, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Summary: The discovery of 5-phenylpyrazolopyrimidinone analogs as a novel series of antitrypanosomal agents shows promise for developing new medications to treat Human African Trypanosomiasis (HAT). The most potent compound, 30, has a low toxicity potential and exhibits high in vitro and in vivo antitrypanosomal activity against T. b. brucei.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Xiangbo Yang, Huimin Lu, Hang Xie, Binbin Zhang, Tianqing Nie, Chen Fan, Tao Yang, Yechun Xu, Haixia Su, Wei Tang, Bing Zhou
Summary: Sepsis, identified by its high risk of life-threatening organ dysfunction, is considered a major cause of health loss, with the World Health Organization labeling it as the most urgent unmet medical need in 2017. The discovery of the role of RIPK1 in sepsis has led to the development of potentially effective therapeutic strategies such as the highly potent compound ZB-R-55, which shows promising therapeutic effects in preclinical studies.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Multidisciplinary
Kris Meier, Josep Arus-Pous, Jean-Louis Reymond
Summary: The study discovered that many chiral, 3D-shaped ring systems, often containing quaternary centers, in the generated databases have not been explored for drug design. By using triquinazine as an example, a nanomolar and selective inhibitor of Janus Kinase 1 was designed, which is related to the marketed drug Tofacitinib used for treating autoimmune diseases.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Biochemistry & Molecular Biology
Ren Kong, Shan Chang, Weiming Xia, Stephen T. C. Wong
JOURNAL OF STRUCTURAL BIOLOGY
(2015)
Article
Biochemistry & Molecular Biology
Lei Xu, Ren Kong, Jingyu Zhu, Huiyong Sun, Shan Chang
MOLECULAR BIOSYSTEMS
(2016)
Article
Biochemistry & Molecular Biology
Ming Liu, Ji Guo Su, Ren Kong, Ting Guang Sun, Jian Jun Tan, Wei Zu Chen, Cun Xin Wang
BIOPHYSICAL CHEMISTRY
(2008)
Article
Oncology
Hong Zhao, Guangxu Jin, Kemi Cui, Ding Ren, Timothy Liu, Peikai Chen, Solomon Wong, Fuhai Li, Yubo Fan, Angel Rodriguez, Jenny Chang, Stephen T. C. Wong
Article
Chemistry, Medicinal
Ya Zhuo, Ren Kong, Xiao-jing Cong, Wei-zu Chen, Cun-xin Wang
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2008)
Article
Medicine, Research & Experimental
Yoo-Shin Kim, Feng Li, Ren Kong, Yang Bai, King C. P. Li, Yubo Fan, Brian E. O'Neill, Zheng Li
MOLECULAR PHARMACEUTICS
(2013)
Article
Multidisciplinary Sciences
Timothy Liu, Ding Ren, Xiaoping Zhu, Zheng Yin, Guangxu Jin, Zhen Zhao, Daniel Robinson, Xuping Li, Kelvin Wong, Kemi Cui, Hong Zhao, Stephen T. C. Wong
SCIENTIFIC REPORTS
(2013)
Article
Biochemistry & Molecular Biology
Lianhua Piao, Zhou Chen, Qiuye Li, Ranran Liu, Wei Song, Ren Kong, Shan Chang
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2019)
Article
Medicine, General & Internal
Xuping Li, Lin Wang, Matthew Cykowski, Tiancheng He, Timothy Liu, Joshua Chakranarayan, Andreana Rivera, Hong Zhao, Suzanne Powell, Weiming Xia, Stephen T. C. Wong
Meeting Abstract
Hematology
Huojun Cao, Zheng Yin, Shenyi Chen, Timothy Liu, Jiyong Liu, Yaping Hu, Hong Zhao, Lawrence Rice, Swaminathan Padmanabhan Iyer, Stephen Wong
Article
Chemistry, Medicinal
Jian Jun Tan, Bin Zhang, Xiao Jing Cong, Lei Fu Yang, Bin Liu, Ren Kong, Zhi Yao Kui, Cun Xin Wang, Li Ming Hu
MEDICINAL CHEMISTRY
(2011)
Article
Biochemistry & Molecular Biology
Ren Kong, Jian Jun Tan, Xiao Hui Ma, Wei Zu Chen, Cun Xin Wang
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS
(2006)