In Situ Bioconjugation of a Maleimide-Functionalized Ruthenium-Based Photosensitizer to Albumin for Photodynamic Therapy

Vinck, Robin and Dömötör, Orsolya and Karges, Johannes and Jakubaszek, Marta and Seguin, Johanne and Tharaud, Mickaël and Guérineau, Vincent and Cariou, Kevin and Mignet, Nathalie and Enyedy, Éva Anna and Gasser, Gilles (2023) In Situ Bioconjugation of a Maleimide-Functionalized Ruthenium-Based Photosensitizer to Albumin for Photodynamic Therapy. INORGANIC CHEMISTRY, 62 (38). pp. 15510-15526. ISSN 0020-1669

Text IC_2023_Gasser.pdf - Published Version Restricted to Registered users only Download (3MB)

Abstract

Maleimide-containing prodrugs can quickly and selectively react with circulating serum albumin following their injection in the bloodstream. The drug–albumin complex then benefits from longer blood circulation times and better tumor accumulation. Herein, we have applied this strategy to a previously reported highly phototoxic Ru polypyridyl complex-based photosensitizer to increase its accumulation at the tumor, reduce off-target cytotoxicity, and therefore improve its pharmacological profile. Specifically, two complexes were synthesized bearing a maleimide group: one complex with the maleimide directly incorporated into the bipyridyl ligand, and the other has a hydrophilic linker between the ligand and the maleimide group.

Actions (login required)

Edit Item