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Synthesis, biological evaluation and molecular docking studies of flavonol-3-O-β-D-glycoside as a potential inhibitor of SARS-CoV-2 main protease (3CLpro) in drug development for COVID-19.
Int J Biol Macromol
January 2025
Department of Basic Medical Sciences, Faculty of Medicine, Istanbul Medipol University, Istanbul 34815, Türkiye.
The COVID-19 pandemic began in March 2020 and has affected many countries and infected over a million people. It has had a serious impact on people's physical and mental health, daily life and the global economy. Today, many drugs show limited efficacy in the treatment of COVID-19 and studies to develop effective drugs continue.
View Article and Find Full Text PDFDiscovery of CZY43 as a new small-molecule degrader of pseudokinase HER3.
Eur J Med Chem
January 2025
State Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd, Shanghai, 200032, China. Electronic address:
The pseudokinase HER3 emerges as a promising anti-cancer target, especially for HER2-driven breast cancer and EGFR-mediated non-small cell lung cancer. However, it is challenging to target HER3 by ATP-competitive small molecules because HER3 is catalytically impaired. Herein, we report the discovery of a series of HER3 degraders by connecting a HER3 binder bosutinib with a hydrophobic tag adamantane.
View Article and Find Full Text PDFImpact of residual aluminum on nanofiltration gypsum scaling: Mitigation roles played by different species.
Water Res
January 2025
State Key Laboratory of Urban Water Resource and Environment, School of Environment, Harbin Institute of Technology, Harbin, 150090, PR China. Electronic address:
Residual aluminum (Al) is a growing pollutant in nanofiltration (NF) membrane-based drinking water treatment. To investigate the impact of distinct Al species fouling layers on gypsum scaling during NF, gypsum scaling tests were conducted on bare and three Al-conditioned (AlCl-, Al, and Al-) membranes. The morphology of gypsum, the role of Al species on Ca adsorption during gypsum scaling, and the interactions between gypsum crystals and Al-conditioned membranes were investigated.
View Article and Find Full Text PDFcolonization is not mediated by bile salts and utilizes Stickland fermentation of proline in an model.
mSphere
January 2025
Department of Food Science and Technology and Nebraska Food for Health Center, University of Nebraska-Lincoln, Lincoln, Nebraska, USA.
Treatment with antibiotics is a major risk factor for infection, likely due to depletion of the gastrointestinal microbiota. Two microbiota-mediated mechanisms thought to limit colonization include the conversion of conjugated primary bile salts into secondary bile salts toxic to growth and competition between the microbiota and for limiting nutrients. Using a continuous flow model that simulates the nutrient conditions of the distal colon, we investigated how treatment with 6 clinically used antibiotics influenced susceptibility to infection in 12 different microbial communities cultivated from healthy individuals.
View Article and Find Full Text PDFHarnessing defective interfering particles and lipid nanoparticles for effective delivery of an anti-dengue virus RNA therapy.
Mol Ther Nucleic Acids
March 2025
Program of Infection and Inflammation, QIMR Berghofer Medical Research Institute, Herston, QLD 4006, Australia.
Currently, no approved antiviral drugs target dengue virus (DENV) infection, leaving treatment reliant on supportive care. DENV vaccine efficacy varies depending on the vaccine type, the circulating serotype, and vaccine coverage. We investigated defective interfering particles (DIPs) and lipid nanoparticles (LNPs) to deliver DI290, an anti-DENV DI RNA.
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