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A self-assembled multivalent glycosidase inhibitor based on perylene bisimide-deoxynojirimycin conjugates was constructed, inhibited α-mannosidase and exhibited a K value of 38 nM, increased approximately 2763-fold compared with the control drug (miglitol). Furthermore, the postprandial blood glucose (PBG) level in mice of PBI-DNJ was firstly studied. PBI-DNJ exhibited a hypoglycaemic effect in vivo. Importantly, this work developed a new means to explore the hypoglycaemic effect in mice based on self-assembled glycosidase inhibitors.
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http://dx.doi.org/10.1039/c8tb03122c | DOI Listing |
Cell Rep
July 2025
Department of Biomedical Engineering, Washington University in St. Louis, St. Louis, MO 63130, USA; Center for Biomolecular Condensates, Washington University in St. Louis, St. Louis MO 63130, USA. Electronic address:
During repeated virus exposure, pre-existing antibodies can mask viral epitopes by competing with B cell receptors for antigen. Although epitope masking has the potential to steer B cell responses away from conserved epitopes and toward those that are antigenically novel, the factors that influence this process remain unclear. Using engineered, influenza-reactive B cells, we investigate how antibodies affect the accessibility of epitopes on the viral surface.
View Article and Find Full Text PDFInt J Biol Macromol
June 2025
College of Chemistry and Chemical Engineering, Shaoxing University, Shaoxing, Zhejiang Province 312000, China. Electronic address:
Enzymes catalyze cascade reactions in a crowded cellular environment where as much as half of cell volume is occupied by various macromolecules. Nonspecific interaction between enzymes and crowders and excluded volume of the crowders can superimpose on each other and complicate catalytic activity of the enzymes. This study investigates the interaction between a β-galactosidase (β-Gal) and glycosylated acrylamide polymer (P(Glc-β-EAAm)) and unravels the macromolecular crowding effect of the glycopolymer on enzymatic cascade catalysis consisting of β-Gal, glucose oxidase and hydrogen peroxidase.
View Article and Find Full Text PDFVaccine
May 2025
Center for Vaccines and Immunology, University of Georgia, Athens, GA, USA; Department of Infectious Diseases, University of Georgia, Athens, GA, USA; Florida Research and Innovation Center, Cleveland, Clinic, Port Saint Lucie, FL, USA; Department of Infection Biology, Lehner Research Institute, Cle
Influenza viruses cause significant mortality in humans, especially among people 65 years and older. The outbreaks of A(H3N2) influenza viruses or viruses of vaccine-mismatched strains are usually associated with more severe diseases in elderly population. Vaccination is the practical countermeasure for controlling influenza virus infection in humans.
View Article and Find Full Text PDFNat Microbiol
April 2025
Cidara Therapeutics, San Diego, CA, USA.
The ability of influenza virus to undergo rapid antigenic shift to elude humoral immunity highlights the need for effective broad-spectrum influenza antivirals for treatment, prophylaxis and pandemic preparedness. Strategies providing durable, universal influenza protection in healthy and high-risk populations are urgently needed. Here we describe the design and preclinical characterization of CD388, a first-in-class antiviral drug-Fc conjugate (DFC), in mice and cynomolgus macaques.
View Article and Find Full Text PDFMolecules
January 2025
Université de Reims Champagne-Ardenne, CNRS, ICMR, 51097 Reims, France.
A straightforward synthetic route towards DAB-1 scaffolded dimeric iminosugars is described here, starting from readily available bis-glycosylamines. The method allows the integration of a variety of linkages (aryl, alkyl, polyethyleneglycol chains) between both iminosugars through the choice of the bis-amine used in the first step. Moreover, an additional substituent (allyl, ethynyl) may be inserted into the structure via nucleophilic addition of an organometallic reagent to the starting bis-glycosylamine.
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