1,2,4-Triazole-Based First-in-Class Non-Nucleoside Inhibitors of the Bacterial Enzyme MraY [0.03%]
一类新的非核苷类细菌MraY酶抑制剂——基于1,2,4-三唑的首创新药抑制剂
Tomayo Berida,Tzu-Yu Huang,Stefanie C Weck et al.
Tomayo Berida et al.
MraY is an essential bacterial enzyme for peptidoglycan synthesis in cell walls and serves as a promising but unrealized target for developing effective antibacterial drugs. Nature has provided a remarkable array of nucleoside inhibitors of...
Functional D- and L‑Naphthalenediimide-Peptides: Microwave-Driven Synthesis, Supramolecular Aggregation, and Multiphoton Fluorescence Lifetime Imaging Microscopy in Living Cells [0.03%]
功能性的D-和L-萘二酰亚胺肽：微波驱动合成、超分子聚集以及活细胞中的多光子荧光寿命成像 microscopy
Simone G Giuffrida,David G Calatayud,Fernando Cortezon-Tamarit et al.
Simone G Giuffrida et al.
We report the microwave-assisted synthesis of a novel family of peptide-linked optical imaging probes incorporating the L-[7,13] bombesin fragment (denoted L-[7,13]-BBN) as a functional building block currently used for targeting the gastri...
Leader-Independent C‑Terminal Modification by a Radical S‑Adenosyl‑l‑methionine Maturase Enables Macrocyclic GLP-1-Like Peptides [0.03%]
不含领导肽的环化GLP-1类似物前体肽的自由基SAM成熟酶介导的末端修饰
Jacob K Pedigo,Karsten A S Eastman,Vahe Bandarian
Jacob K Pedigo
Ribosomally synthesized and post-translationally modified peptides (RiPPs) are a rapidly expanding family of natural products in which biosynthetic maturase enzymes tailor ribosomal precursors into bioactive products. Classical RiPP maturat...
Manipulation of 7‑Finger Zinc Finger Nuclease Increases the Efficiency of Genome Editing in Human Cells [0.03%]
利用7指锌指核酸酶提高人类细胞的基因组编辑效率
Shota Katayama,Masahiro Watanabe,Wataru Nomura et al.
Shota Katayama et al.
Genome editing tools have great potential for medicinal use. Among them, zinc finger nucleases (ZFNs) are smaller in size than transcriptional activator-like effector nucleases and CRISPR-Cas9. Therefore, ZFNs are easily packed into a viral...
High-Throughput Microfluidic Technologies for Rapidly Screening Pollutant-Induced Cell Health Effects [0.03%]
高通量微流控技术快速筛查污染物引起的细胞健康效应
Blanca I Quiñones-Díaz,Niphattha Wongwiset,Pratik Kamat et al.
Blanca I Quiñones-Díaz et al.
Air pollution exposure is linked to diseases spanning multiple physiological systems. However, environmental stress is overwhelmingly associated with several lung diseases. Since the chemical composition of air pollutants varies widely acro...
Malkeet Kumar,Anees Ahmad,Anna Caroline Campos Aguiar et al.
Malkeet Kumar et al.
Malaria still stands out as one of the most devastating and prevalent diseases globally, where the rise of resistance to different antimalarial drugs in different regions has posed significant obstacles to global treatment and elimination. ...
Synthesis of a Water-Soluble BODIPY for Targeting and Assessing the Function of Endoplasmic Reticulum [0.03%]
用于内质网靶向及功能评估的水溶性BODIPY染料的合成
Jacopo Tricomi,Giacomo Biagiotti,Tommy Chastel et al.
Jacopo Tricomi et al.
We report here on a straightforward methodology to synthesize a new water-soluble fluorescent probe Tris-BODIPY-OH 1 that contains three pH-independent hydrophilic arms. This probe has been prepared by exploiting a synthetic strategy that i...
Targeted Protein Degradation for Agricultural Applications: Rationale, Challenges, and Outlook [0.03%]
靶向蛋白质降解在农业应用中的作用：原理、挑战与前景
Denis Fourches,Joseph Pilotte,Brian E Watts et al.
Denis Fourches et al.
Farmers urgently need novel technologies to ensure global food security for the rapidly expanding population, yet crop protection has seen little innovation in decades. Mounting regulatory pressures, pest resistance, and environmental conce...
Transition State Analysis of the Aldol-Like Reaction Catalyzed by NeuB, a Sialic Acid Synthase, Reveals a Stepwise Cationic Mechanism [0.03%]
神经氨酸合成酶NeuB催化的类似aldol反应的过渡态分析揭示了逐步阳离子机制
Pallavi Mukherjee,Chen Niu,Paul J Berti
Pallavi Mukherjee
The sialic acid synthase NeuB, and other α-carboxyketose synthases, are long-standing targets for inhibition by potential antimicrobial compounds. NeuB catalyzes an aldol-like reaction of phosphoenolpyruvate (PEP) and N-acetylmannosamine (...
Allosteric Modulation of Cannabinoid Type 1 Receptor by ZCZ011: Integration of In Vitro Pharmacology and Molecular Dynamics Simulation [0.03%]
allosteric调节剂ZCZ011对大麻素受体1的药理学及分子动力学研究
Tara Chand Yadav,Lakshmipriya Indira Swaminathan,Venkat R Chirasani et al.
Tara Chand Yadav et al.
Over the years, the cannabinoid type 1 receptor (CB1R) has emerged as a promising therapeutic target for addressing various neurodegenerative diseases including HIV-associated neurocognitive disorders (HAND). However, the therapeutic applic...