Results 61 to 70 of about 38,167 (247)

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad‐Spectrum Antiviral Activity

Advanced Science, EarlyView.
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Weilong Deng, Junyu Chen, Yingyue Pang, Yuanyuan Zhang, Siqian Chen, Guoliang You, Xiaoman Tian, Zhongxin Xu, Jing Wang, Luqing Shang   +9 more
wiley   +1 more source

Prolonged Infusion of β-Lactams Decreases Mortality in Patients with Septic Shock: A Retrospective before-and-after Study

Antibiotics, 2021
Septic shock substantially alters the pharmacokinetic properties of β-lactams with a subsequently high risk of insufficiently low serum concentrations and treatment failure.
Daniel Christoph Richter, Maximilian Dietrich, Lazar Detelinov Lalev, Felix C. F. Schmitt, Mascha Onida Fiedler, Thomas Bruckner, Dominic Stoerzinger, Ute Chiriac, Sabrina Klein, Thilo Hackert, Thorsten Brenner, Alexander Brinkmann, Markus A. Weigand   +12 more
doaj   +1 more source

High‐Density E. Coli Cultivation Arrays for Combinatorial Drug Testing With Subsequent Lipid Profiling by MALDI‐MS

Advanced Science, EarlyView.
High‐throughput antibiotic cross‐gradient assays on microdroplet arrays. A multichannel printhead together with five pressure regulators forms droplet arrays of up to 20 832 droplets within 25 minutes. Each droplet contains unique concentrations of antibiotics, allowing to moniture a vast spectrum of bacterial repsonses over night. The bacterial growth
M. Breitfeld, C. L. Dietsche, F‐L. Born, I. Onipko, L. Blaase, P. S. Dittrich   +5 more
wiley   +1 more source

Electron Donor–Acceptor Complex Catalysis in Synthetic Chemistry

Angewandte Chemie, EarlyView.
Electron donor–acceptor (EDA) complexes are moving beyond stoichiometric photoactivation toward catalytic platforms for radical generation. Productive EDA catalysis requires coordinated donor–acceptor association, charge‐transfer excitation, radical reactivity, and vcatalyst turnover.
Tristan von Münchow, Andrea Palone, Jonathan Samuel Trimble, Paolo Melchiorre   +3 more
wiley   +2 more sources

Mycobacterium abscessus and β-Lactams: Emerging Insights and Potential Opportunities

Frontiers in Microbiology, 2018
β-lactams, the most widely used class of antibiotics, are well-tolerated, and their molecular mechanisms of action against many bacteria are well-documented.
Elizabeth Story-Roller, Emily C. Maggioncalda, Keira A. Cohen, Gyanu Lamichhane   +3 more
doaj   +1 more source

Pyrazole‐Derived Antibacterial Compounds Effectively Treat Methicillin‐Resistant Staphylococcus Aureus Infections by Inhibiting Aspartate Transcarbamoylase

Advanced Science, EarlyView.
This study unveils a novel antibacterial mechanism against MRSA, in which the compound Py‐27 selectively targets and inhibits aspartate transcarbamoylase (ATCase), a key enzyme in pyrimidine synthesis. This inhibition disrupts DNA replication, induces oxidative damage, leading to potent bactericidal activity.
Xiaorong Yang, Xinyuan Cao, Lixia Dai, Feng Yang, Jing Wang, Yudong Ma, Tong Bu, Zile Gong, Xueyan Liu, Changcai Bai, Xiaolou Miao, Xiaofei Shang   +11 more
wiley   +1 more source

Switching ATP‐Forming Phosphoryl‐Transfer Chemistry With a Restricted Set of Amino Acids

Angewandte Chemie, EarlyView.
Constraints on amino acid composition relevant to prebiotic chemistry reshape enzyme chemistry by replacing the canonical mechanism within a conserved protein fold with a distinct ATP‐forming reaction, ADP disproportionation. Such constraints generate alternative catalytic solutions not observed in modern enzymes and point to chemically plausible early
Sota Yagi, Subrata Dasgupta, Shunsuke Tagami, Satoshi Akanuma   +3 more
wiley   +2 more sources

Structural comparison of substrate-binding pockets of serine β-lactamases in classes A, C, and D

Journal of Enzyme Inhibition and Medicinal Chemistry
β-lactams have been the most successful antibiotics, but the rise of multi-drug resistant (MDR) bacteria threatens their effectiveness. Serine β-lactamases (SBLs), among the most common causes of resistance, are classified as A, C, and D, with numerous ...
Hyeonmin Lee, Hyunjae Park, Kiwoong Kwak, Chae-eun Lee, Jiwon Yun, Donghyun Lee, Jung Hun Lee, Sang Hee Lee, Lin-Woo Kang   +8 more
doaj   +1 more source

Asymmetric Single‐Atom Catalysts Govern Diffusible and Non‐Diffusible Non‐Radical Pathways for Selective Degradation of Antibiotic Resistance Genes

Advanced Science, EarlyView.
Asymmetric single‐atom metal‐nitrogen‐carbon catalysts modulate the non‐radical pathway during peroxymonosulfate (PMS) activation. A fundamental contrast was revealed between diffusible singlet oxygen (1O2) and non‐diffusible electron‐transfer pathways (ETP) in antibiotic resistance gene (ARG) degradation.
Chen Gao, Jun Sun, Liang Zhang, Litao Lin, Zongfeng Wan, Bingcai Pan, Sheng Tang   +6 more
wiley   +1 more source

Structure and Biosynthesis of Mangotoxin Produced by the Plant Pathogen Pseudomonas syringae

Angewandte Chemie, EarlyView.
The structure of mangotoxin remained elusive for over two decades. Here, mangotoxin was isolated from the native producer, Pseudomonas syringae pv. syringae, and was determined to be an alkyne‐containing dipeptide. Mangotoxin inhibited the growth of multidrug‐resistant human pathogen Klebsiella pneumoniae.
Alexis H. Murray, Sohan Hazra, Ryan W. Mull, Erinn M. O'Neill, Bo Li   +4 more
wiley   +2 more sources