Fiche publication
Date publication
juin 2018
Journal
Angewandte Chemie (International ed. in English)
Auteurs
Membres identifiés du Cancéropôle Est :
Pr DENAT Franck
,
Dr GONCALVES Victor
Tous les auteurs :
Canovas C, Moreau M, Bernhard C, Oudot A, Guillemin M, Denat F, Goncalves V
Lien Pubmed
Résumé
Dual-labeled biomolecules constitute a new generation of bioconjugates with promising applications in therapy and diagnosis. Unfortunately, the development of these new families of biologics is hampered by the technical difficulties associated with their construction. In particular, achieving site-specific labeling of proteins is critical as the number and position of payloads can have a dramatic impact on the pharmacokinetic of the bioconjugate. Here, we introduce dichloro-tetrazine as a trivalent platform for the selective double-modification of proteins on cysteine residues. This strategy is applied to the dual-labeling of albumin with a macrocyclic chelator for nuclear imaging and a fluorescent probe for fluorescence imaging.
Mots clés
bioconjugation, click chemistry, cysteine, protein engineering, site-specific labeling
Référence
Angew. Chem. Int. Ed. Engl.. 2018 Jun 15;:
