Fiche publication


Date publication

mars 2023

Journal

Journal of medicinal chemistry

Auteurs

Membres identifiés du Cancéropôle Est :
Pr PAUL Catherine , Pr DENAT Franck


Tous les auteurs :
Godard A, Kalot G, Privat M, Bendellaa M, Busser B, Wegner KD, Denat F, Le Guével X, Coll JL, Paul C, Bodio E, Goze C, Sancey L

Résumé

Using fluorescence-guided surgery (FGS) to cytoreductive surgery helps achieving complete resection of microscopic ovarian tumors. The use of visible and NIR-I fluorophores has led to beneficial results in clinical trials; however, involving NIR-II dyes seems to outperform those benefits due to the deeper tissue imaging and higher signal/noise ratio attained within the NIR-II optical window. In this context, we developed NIR-II emitting dyes targeting human epidermal growth factor receptor 2 (HER2)-positive ovarian tumors by coupling water-soluble NIR-II aza-BODIPY dyes to the FDA-approved anti-HER2 antibody, namely, trastuzumab. These bioconjugated NIR-II-emitting dyes displayed a prolonged stability in serum and a maintained affinity toward HER2 in vitro. We obtained selective targeting of HER2 positive tumors (SKOV-3) in vivo, with a favorable tumor accumulation. We demonstrated the fluorescence properties and the specific HER2 binding of the bioconjugated dyes in vivo and thus their potential for NIR-II FGS in the cancer setting.

Référence

J Med Chem. 2023 03 30;: