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Structural fine-tuning of desmuramylpeptide NOD2 agonists defines their in vivo adjuvant activityGuzelj, Samo ...We report on the design, synthesis, and biological evaluation of a series of nucleotide-binding oligomerization-domain-containing protein 2 (NOD2) desmuramylpeptide agonists with improved in vitro ... and in vivo adjuvant properties. We identified two promising compounds: 68, a potent nanomolar in vitro NOD2 agonist, and the more lipophilic 75, which shows superior adjuvant activity in vivo. Both compounds had immunostimulatory effects on peripheral blood mononuclear cells at the protein and transcriptional levels, and augmented dendritic-cell-mediated activation of T cells, while 75 additionally enhanced the cytotoxic activity of peripheral blood mononuclear cells against malignant cells. The C18 lipophilic tail of 75 is identified as a pivotal structural element that confers in vivo adjuvant activity in conjunction with a liposomal delivery system. Accordingly, liposome-encapsulated 75 showed promising adjuvant activity in mice, surpassing that of muramyl dipeptide, while achieving a more balanced Th1/Th2 immune response, thus highlighting its potential as a vaccine adjuvant.Source: Journal of medicinal chemistry. - ISSN 0022-2623 (Vol. 64, iss. 11, 2021, str. 7809-7838)Type of material - article, component partPublish date - 2021Language - englishCOBISS.SI-ID - 64930051
Author
Guzelj, Samo |
Nabergoj, Sanja |
Gobec, Martina, 1983- |
Pajk, Stane, 1983- |
Klančič, Veronika |
Slütter, Bram |
Frkanec, Ruža |
Štimac, Adela |
Šket, Primož, 1977- |
Plavec, Janez |
Mlinarič-Raščan, Irena |
Jakopin, Žiga
Topics
Farmacevtska kemija |
Peptidi |
Toksičnost |
Organske spojine |
reakcijski produkti |
reaction products |
peptides and proteins |
cells |
organic compounds |
toxicity
Author | Guzelj, Samo ... |
Title | Structural fine-tuning of desmuramylpeptide NOD2 agonists defines their in vivo adjuvant activity |
Publication date | 2021-05-29 |
COBISS.SI-ID | 64930051 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution-NonCommercial 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Razvoj agonistov receptorja NOD2 ter dualnih NOD2/TLR7 agonističnih konjugatov kot novih adjuvansov za cepiva | J3-9256-2018 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
Files that belong to the publication
Link |
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https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c00644 |
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=141424 |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Guzelj, Samo | 52379 |
Nabergoj, Sanja | 38165 |
Gobec, Martina, 1983- | 32034 |
Pajk, Stane, 1983- | 28861 |
Klančič, Veronika | 54787 |
Slütter, Bram | |
Frkanec, Ruža | |
Štimac, Adela | |
Šket, Primož, 1977- | 22575 |
Plavec, Janez | 10082 |
Mlinarič-Raščan, Irena | 12443 |
Jakopin, Žiga | 26496 |
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