Glycan shields for penetrating peptides
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Título: | Glycan shields for penetrating peptides |
Autor/a: | Gallego Gómez, Iván Montenegro García, Javier |
Centro/Departamento: | Universidade de Santiago de Compostela. Centro de Investigación en Química Biolóxica e Materiais Moleculares Universidade de Santiago de Compostela. Departamento de Química Orgánica |
Data: | 2021 |
Editor: | Royal Society of Chemistry |
Cita bibliográfica: | Chem. Commun., 2022,58, 1394-1397 |
Resumo: | We here describe the synthesis and biological evaluation of glycan shields for cell penetrating peptides. A new benzyl alkoxyamine connector was employed for the coupling of two saccharides units in the lateral side chain of individual amino acids in a peptide sequence. The oxyme bond formation with the corresponding glycan aldehydes allowed the preparation of highly glycosylated penetrating peptides with a minimal synthetic effort. Surprisingly, it was found that a four to six saccharide substitution did not decrease uptake efficiency in cells, whereas it significantly improved the toxicity profile of the penetrating peptide. In particular, glucose substitution was confirmed as an optimal glycan shield that showed an excellent in vitro uptake and intracellular localization as well as a superior in vivo biodistribution |
Versión do editor: | https://doi.org/10.1039/D1CC06252B |
URI: | http://hdl.handle.net/10347/29371 |
DOI: | 10.1039/D1CC06252B |
ISSN: | 0009-241X |
E-ISSN: | 2050-5620 |
Dereitos: | © Royal Society of Chemistry, 2021 |
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