Fiche publication
Date publication
juillet 2015
Auteurs
Membres identifiés du Cancéropôle Est :
Dr BAGNARD Dominique
,
Dr MULLER Christian
,
Dr WAGNER Alain
Tous les auteurs :
Leriche G, Nothisen M, Baumlin N, Muller CD, Bagnard D, Remy JS, Jacques SA, Wagner A
Lien Pubmed
Résumé
pH-sensitive linkers designed to undergo selective hydrolysis at acidic pH compared to physiological pH can be used for selective release of therapeutics selectively at targets and orthoesters have demonstrated to be good candidate for such linkers. Following an HPLC screen, a Spiro Di-orthoester (SpiDo) derivative was identified as a potent acid-labile group for the development of pH-sensitive targeted systems. After incorporation of this linker into activatable FRET-based probe and side-by-side comparison to a well-known alkylhydrazone linker, this SpiDo linker has shown a fast and pH sensitive hydrolysis for mild acidic conditions, a pH sensitive lysosomal hydrolysis and a high stability in Human plasma.
Référence
Bioconjug Chem. 2015 Jul 1.
