The synthesis of two polyhydroxylated pyrrolidines as 1,4-dideoxy-1,4-imino-d-arabinitol (DAB) analogues bearing a hydrazide moiety is described. The DAB analogues act as selective and potent inhibitors of α-mannosidase in the submicromolar concentration ranges ( values ranging from 0.23 to 1.4 μM).
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http://dx.doi.org/10.1021/acsomega.0c02466 | DOI Listing |
Commun Biol
October 2024
CAS Key Laboratory of Marine Ecology and Environmental Sciences, Institute of Oceanology, Chinese Academy of Sciences, Qingdao, 266071, China.
Front Pharmacol
October 2024
ACTV Research Group, Melbourne Dental School, Division of Basic and Clinical Oral Sciences, Royal Dental Hospital and The Bio21 Institute of Molecular Science and Biotechnology, The University of Melbourne, Melbourne, VIC, Australia.
Introduction: Melittin is a potent antimicrobial peptide from bee venom that is effective against both Gram-positive and Gram-negative bacteria. However, it is extremely toxic to mammalian cells and, as yet, has no clinical use. Modifications to its amino acid sequence, cyclization, truncation, and dimerization have been attempted in order to reduce its toxicity whilst maintaining its antimicrobial activity.
View Article and Find Full Text PDFEcotoxicol Environ Saf
October 2024
UPR CHROME (Risques CHROniques et eMErgents), University of Nîmes, Nîmes, France. Electronic address:
The increasing concern over the environmental presence of β-N-Methylamino-L-alanine (BMAA), a toxin primarily produced by cyanobacteria and diatoms, has stimulated numerous studies to evaluate the risk for exposed populations, mainly aquatic organisms and humans. This study focuses on the toxicity of environmental concentrations of BMAA and its isomers, l-2,4 diaminobutyric acid dihydrochloride (DAB) and N-(2-aminoethyl) glycine (AEG) on zebrafish embryo development (ng.L).
View Article and Find Full Text PDFProc Natl Acad Sci U S A
October 2024
Microbial and Environmental Genomics Group, J. Craig Venter Institute, La Jolla, CA 92037.
In 2015, the largest recorded harmful algal bloom (HAB) occurred in the Northeast Pacific, causing nearly 100 million dollars in damages to fisheries and killing many protected marine mammals. Dominated by the toxic diatom , this bloom produced high levels of the neurotoxin domoic acid (DA). Through molecular and transcriptional characterization of 52 near-weekly phytoplankton net-tow samples collected at a bloom hotspot in Monterey Bay, California, we identified active transcription of known DA biosynthesis () genes from the three identified toxigenic species, including as the primary origin of toxicity.
View Article and Find Full Text PDFAmino Acids
August 2024
Faculty of Chemistry, University of Warsaw, Pasteura 1, 02-093, Warsaw, Poland.
Inhibitors of the interaction between Neuropilin-1 (NRP-1) and Vascular Endothelial Growth Factor-A (VEGF-A) hold significant promise as therapeutic and diagnostic agents directed against cancers overexpressing NRP-1. In our efforts in this field, a few series of strong and fairly stable peptide-like inhibitors of the general formula Lys(Har)-Xaa-Xaa-Arg have been previously discovered. In the current work, we focused on Lys(Har)-Dap/Dab-Pro-Arg sequence.
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