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We developed a design strategy focusing on pivotal secondary structural motifs-α-helix, β-strand, and β-turn-critical for PPI recognition, using a common core skeleton. The resulting peptide-inspired pyrimidodiazepine scaffolds were further subjected to comprehensive phenotypic screening to evaluate their efficacy. Our strategy offers a transformative approach to developing small-molecule PPI modulators with broad therapeutic potential.
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http://dx.doi.org/10.1039/d4cc06630h | DOI Listing |
FEMS Microbiol Rev
September 2025
CIISA - Centre for Interdisciplinary Research in Animal Health, Faculty of Veterinary Medicine, University of Lisbon, Lisbon, Portugal.
African Swine Fever (ASF), caused by the highly contagious African swine fever virus (ASFV), poses a significant threat to domestic and wild pigs worldwide. Despite its limited host range and lack of zoonotic potential, ASF has severe socio-economic and environmental consequences. Current control strategies primarily rely on early detection and culling of infected animals, but these measures are insufficient given the rapid spread of the disease.
View Article and Find Full Text PDFJ Am Chem Soc
September 2025
State Key Laboratory of Supramolecular Structure and Materials, College of Chemistry, Jilin University, Changchun 130012, China.
Metal-organic frameworks (MOFs) are distinguished by their structural diversity, tunable electronic properties, and exceptional performance in various applications. Notably, the electron-donating ability of ligands significantly enhances the ligand-to-metal charge transfer (LMCT) processes within these frameworks, thereby promoting efficient charge migration. Herein, we developed two electron-rich macrocyclic ligands derived from phenothiazine- and phenoxazine-functionalized calix[3]arenes, alongside their corresponding cobalt-coordinated MOFs.
View Article and Find Full Text PDFACS Chem Neurosci
September 2025
Chemical and Biomolecular Engineering Dept, University of California, Los Angeles, Los Angeles, California 90095, United States.
Simulations in three dimensions and time provide guidance on implantable, electroenzymatic glutamate sensor design; relative placement in planar sensor arrays; feasibility of sensing synaptic release events; and interpretation of sensor data. Electroenzymatic sensors based on the immobilization of oxidases on microelectrodes have proven valuable for the monitoring of neurotransmitter signaling in deep brain structures; however, the complex extracellular milieu featuring slow diffusive mass transport makes rational sensor design and data interpretation challenging. Simulations show that miniaturization of the disk-shaped device size below a radius of ∼25 μm improves sensitivity, spatial resolution, and the accuracy of glutamate concentration measurements based on calibration factors determined .
View Article and Find Full Text PDFTop Curr Chem (Cham)
September 2025
Center for Advanced Materials Research, Research Institute of Sciences and Engineering, University of Sharjah, 27272, Sharjah, United Arab Emirates.
Controlling the size of gold nanoparticles (AuNPs) has been critical in diagnostics, biomolecular sensing, targeted therapy, wastewater treatment, catalysis, and sensing applications. Ultrasmall AuNPs (uAuNPs), with sizes Ranging from 2 to 5 nm, and gold nanoclusters (AuNCs), with sizes less than 2 nm, are often dealt with interchangeably in the literature, making it challenging to review them separately. Although they are grouped in our discussion, their chemical and physical properties differ significantly, partly due to their electronic properties.
View Article and Find Full Text PDFJ Antimicrob Chemother
September 2025
Department of Pharmaceutical Sciences, University of Michigan College of Pharmacy, Ann Arbor, MI 48109, USA.
Background: Synergy between antibiotic pairs is typically discovered using chequerboard assays that assume uniform, static drug exposure; however, such conditions rarely apply in vivo. Dynamic and heterogeneous tissue environments create spatial and temporal mismatches in drug exposure that can uncouple synergistic interactions, leading to unexpected treatment failure.
Objective: This study aims to develop a physiologically relevant in vitro model that integrates infection-site microenvironments and drug-specific pharmacokinetics.