Several 7-aminoamido-pterins were synthesized to evaluate the electronic and biochemical subtleties observed in the 'linker space' when N-{N-(pterin-7-yl)carbonylglycyl}-l-phenylalanine 1 was bound to the active site of RTA. The gylcine-phenylalanine dipeptide analogs included both amides and thioamides. Decarboxy gly-phe analog 2 showed a 6.4-fold decrease in potency (IC50 = 128 μM), yet the analogous thioamide 7 recovered the lost activity and performed similarly to the parent inhibitor (IC50 = 29 μM). Thiourea 12 exhibited an IC50 nearly six times lower than the oxo analog 13. All inhibitors showed the pterin head-group firmly bound in their X-ray structures yet the pendants were not fully resolved suggesting that all pendants are not firmly bound in the RTA linker space. Calculated log P values do not correlate to the increase in bioactivity suggesting other factors dominate.
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http://dx.doi.org/10.1016/j.bmcl.2013.10.017 | DOI Listing |
Swiss J Geosci
December 2024
Department of Surface Waters Research and Management, Eawag, Überlandstrasse 133, Dübendorf, 8600 Switzerland.
Unlabelled: Industrial activities of a silk dyeing factory in Thalwil, on the shore of Lake Zurich, Switzerland, caused extreme Sn contamination of lake sediments. In this study, we determine the contamination source, spread, and age using a multiproxy approach. We used X-ray fluorescence spectroscopy (XRF) core scanning and further geochemical analyses to assess the contamination spreading and thickness in the sedimentary column.
View Article and Find Full Text PDFJ Phys Chem B
December 2024
Department of Chemistry, Faculty of Science, Kasetsart University, Chatuchak, Bangkok 10900, Thailand.
Human carnosinases (CNs) are Xaa-His metal-ion-activated aminopeptidases that break down bioactive carnosine and other histidine-containing dipeptides. Carnosine is a bioactive peptide found in meat and prevalently used as a supplement and in functional food formulation. Nonetheless, carnosine is digested by CNs rapidly after ingestion.
View Article and Find Full Text PDFPLoS One
October 2024
Department of Radioecological and Biodosimetric Research, Brunch "Institute of Radiation Safety and Ecology" of National Nuclear Center of Republic of Kazakhstan, Kurchatov, Abay region, Kazakhstan.
During the period from 2019 to 2021, a series of experiments were carried out to study the uptake of tritium by crops in an area heavily contaminated with atmospheric tritium oxide (HTO), at the former Semipalatinsk test site in Kazakhstan. A quantitative assessment is given of the tritium uptake by typical crops (lettuce, tomatoes, peppers and beans) cultivated all over Kazakhstan in the case of a short-term tritium oxide vapor exposure. The plant samples were collected during and after exposure and analyzed for the tritium concentration in two chemical forms: tissue-free water tritium (TFWT) and organically bound tritium (OBT).
View Article and Find Full Text PDFInt J Parasitol Parasites Wildl
December 2024
Papanin Institute for Biology of Inland Waters, Russian Academy of Sciences, 152742, Borok, Yaroslavl District, Russia.
The caryophyllidean tapeworm (Janiszewska, 1953) is indigenous to the Lake Blidinje in the west-central part of Bosnia-Herzegovina where it infects chub (Heckel, 1843). Of 22 chubs examined, 45% were infected with and a total of 912 specimens of this worm were counted. Histopathological and ultrastructural investigations were conducted on interface region between chub intestine and cestode scolex.
View Article and Find Full Text PDFInt J Biol Macromol
November 2024
Guangxi Key Laboratory of Special Biomedicine, School of Medicine, Guangxi University, Nanning 530004, China. Electronic address:
Over the past few decades, research on cancer immunotherapy has firmly established immune cells as key players in effective cancer treatment. Peptide vaccines directly targeting immune cells have demonstrated immense potential due to their specificity and applicability. However, developing peptide vaccines to generate tumor-reactive T cells remains challenging, primarily due to suboptimal immunogenicity and overcoming the immunosuppressive tumor microenvironment (TME).
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