Results 71 to 80 of about 32,790 (255)

Conformational Snapshots of CydDC in a Native Lipid Bilayer Coupling Heme Transport to Antibiotic Resistance

Advanced Science, EarlyView.
Phylogenetic and biochemical analyses of the heme transporter CydDC reveal its functional conservation throughout bacterial evolution and demonstrate its unique asymmetric allosteric mechanism. Furthermore, impairment of CydDC function directly affects bacterial antibiotic resistance and likely compromises antibiotic efficacy through drug efflux.
Lili Yang, Changbin Zhang, Mengyuan Lyu, Yongbo Luo, Jierou Zhang, Yujiao Chen, Lintao Luo, Wen Qiao, Xiangyangpeng Li, Yu Zhou, Zhongling Wei, Yuling Xiao, Qian Niu, Juan Zhou, Guanglin He, Binwu Ying, Zhaoming Su, Hao Chen, Xiaodi Tang, Haohao Dong   +19 more
wiley   +1 more source

Identification of a Nonribosomal Peptide Analog With Activity Against Multiple Gram‐Positive Bacteria via a Synthetic Bioinformatic Natural Product Discovery Approach

Advanced Science, EarlyView.
The genome of Rhodococcus erythropolis D‐1 was analyzed by bioinformatic tools to mine a novel nonribosomal peptide synthetase (NRPS) gene cluster. A nonribosomal peptide analog ZURJC5 associated with the NRPS was chemically synthesized. Through structure‐activity relationship studies, ZURJC28 was ultimately obtained and showed antibacterial activity ...
Keyi Chen, Jiayi Liang, Yujia Wu, Jianan Xu, Yi Liu, Wenguang Wang, Xinhang Jiang, Benjie Gao, Yueyue Wang, Hui Jiang   +9 more
wiley   +1 more source

Quantitative Structure Activity Relationship Studies of Topoisomerase I Inhibitors as Potent Antibreast Cancer Agents

Journal of Chemistry, 2013
Topoisomerase I (TOP I) is a valuable molecular target for the development of clinically used anticancer agents. Indenoisoquinolines have emerged as potent topoisomerase I inhibitors.
Supriya Singh, Sucheta Das, Anubhuti Pandey, Sarvesh Paliwal, Rajeev Singh   +4 more
doaj   +1 more source

Regulation of the Aurora-A gene following topoisomerase I inhibition: implication of the Myc transcription Factor

Molecular Cancer, 2010
During the G2 phase of the cell cycle, the Aurora-A kinase plays an important role in centrosome maturation and progression to mitosis. In this study, we show in colorectal cell lines that Aurora-A expression is downregulated in response to topoisomerase
Valo Isabelle, Giraud Sandrine, Troadec Marie-Bérangère, Vigneron Arnaud, Cherier Julia, Courapied Sandy, Prigent Claude, Gamelin Erick, Coqueret Olivier, Barré Benjamin   +9 more
doaj   +1 more source

Hybrid Inhibitors of DNA Gyrase A and B: Design, Synthesis and Evaluation

Pharmaceutics, 2020
The discovery of multi-targeting ligands of bacterial enzymes is an important strategy to combat rapidly spreading antimicrobial resistance. Bacterial DNA gyrase and topoisomerase IV are validated targets for the development of antibiotics.
Martina Durcik, Žiga Skok, Janez Ilaš, Nace Zidar, Anamarija Zega, Petra Éva Szili, Gábor Draskovits, Tamás Révész, Danijel Kikelj, Akos Nyerges, Csaba Pál, Lucija Peterlin Mašič, Tihomir Tomašič   +12 more
doaj   +1 more source

Accelerating Primary Screening of USP8 Inhibitors from Drug Repurposing Databases with Tree‐Based Machine Learning

Advanced Intelligent Discovery, EarlyView.
This study introduces a tree‐based machine learning approach to accelerate USP8 inhibitor discovery. The best‐performing model identified 100 high‐confidence repurposable compounds, half already approved or in clinical trials, and uncovered novel scaffolds not previously studied. These findings offer a solid foundation for rapid experimental follow‐up,
Yik Kwong Ng, Sharon Ai Er Lam, Wei Chun Lim, Hannah Hui Min Toh, Shi Jun Ang   +4 more
wiley   +1 more source

Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors

, 2016
Designing multitarget drugs remains a significant challenge in current antitumor drug discovery. Because of the synergistic effect between topoisomerase and HDAC inhibitors, the present study reported the first-in-class triple inhibitors of topoisomerase
Chunquan Sheng (1364184), Zhibin Wang (1414969), Zhenyuan Miao (1364187), Wannian Zhang (1364172), Jianzhong Yao (1364175), Guoqiang Dong (1364169), Yahui Huang (1638778), Na Liu (102929), Zhengang Li (714519), Shipeng He (1638781), Wei Chen (23863), Yan Jiang (12139)   +11 more
core   +1 more source

Integrating One Health to Mitigate the Emergence and Spread of Antimicrobial Resistance in Livestock and Aquaculture

Animal Research and One Health, EarlyView.
Antimicrobial resistance (AMR) is an escalating global threat driven by antimicrobial use in aquaculture and livestock. Resistant pathogens and genes can spread across humans, animals, and the environment through interconnected ecosystems. Using a One Health approach, this review emphasizes antimicrobial stewardship, regulatory strengthening, enhanced ...
Mir Mohammad Ali, Delower Hossain, Ridwan Olamilekan Adesola, Anum Hanif, Shamsaldeen Ibrahim Saeed, Muhammad Abdul Mannan, Anoar Jamai Masroure, Kazi Estieque Alam, Md Kamal Hossain, Sabiha Zarin Tasnim Bristi, Md Jisan Ahmed   +10 more
wiley   +1 more source

Structure Guided Design of Xanthomonas oryzae pv. oryzae Topoisomerase I Inhibitors

Proceedings, 2017
Topoisomerase inhibitors initiate the cell killing process by either stabilizing or increasing the amount of the covalent complex formed between the enzyme and cleaved DNA. [...]
Lakindu Samaranayake P. K., Inoka C. Perera   +1 more
doaj   +1 more source

Integrated Clinical and Proteomic Profiling of CD19 Chimeric Antigen Receptor T Cell Therapy in Progressive Systemic Sclerosis

Arthritis &Rheumatology, EarlyView.
Objective To characterize the clinical, immunologic, and proteomic changes associated with CD19 chimeric antigen receptor T cell therapy in patients with progressive systemic sclerosis (SSc). Methods Patients with progressive SSc received CD19 chimeric antigen receptor (CAR)‐T cell therapy and were observed longitudinally for safety, clinical efficacy,
Chenhan Jia, Wanyi Lin, Zhangyi Zhao, Fenglin Wu, Chaoyu Gu, Yuankai Sun, Zhe Ding, Chang Wei, Xinyu Li, Cuiwei Xie, Peng Xia, Zhen Xia, Xuesong Liu, Shaoying Yang, Chunyan Zhang, Hanlin Yin, Liangjing Lu   +16 more
wiley   +1 more source