1335002-97-5Relevant articles and documents
GLYCOSIDE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF AS PROSTHETIC GROUPS
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Paragraph 0096-0099, (2016/04/02)
The present invention relates to glycoside-derived compounds, to the processes for preparing same and to the use thereof as prosthetic groups for radiolabelling biomolecules. These compounds are co-azido-alkyl 6-deoxy-6-[18F]-fluoroglycosides of formula (I), in which: k is equal to 2 or 3; n is an integer between 1 and 5; R is independently H or a C1-C5 alkyl group, m being an integer between 0 and 2 if k=2 and m between 0 and 3 if k=3; and X is chosen from the group comprising O, S, CH2 and NR′, in which R′ is independently a C1-C5 alkyl group or an aryl group, including all the stereoisomers thereof.
Click glycosylation of peptides through cysteine propargylation and CuAAC
Lamandé-Langle, Sandrine,Collet, Charlotte,Hensienne, Rapha?l,Vala, Christine,Chrétien, Fran?oise,Chapleur, Yves,Mohamadi, Amel,Lacolley, Patrick,Regnault, Véronique
, p. 6672 - 6683 (2015/02/19)
'Click' glycosylation of cysteine-containing peptides were carried out in good yield by Copper(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC). For that peptides were functionalized though direct propargylation of the cysteine residue allowing their use in CuAAC with suitable free or protected azido sugars of gluco, manno and galacto configuration. Among these free and protected glycopeptides a series of 'glycoRGD' peptides were obtained and submitted to in vitro platelet aggregation tests, showing that the pseudoglycosylation of the adhesion sequence lowers the IC50 value and thus could improve the in vivo pharmacokinetic properties.
