Cyclic Ruthenium-Peptide Conjugates as Integrin-Targeting Phototherapeutic Prodrugs for the Treatment of Brain Tumors

• Published in: Journal of the American Chemical Society Vol. 145; no. 27; pp. 14963 - 14980
• Main Authors: Zhang, Liyan, Wang, Peiyuan, Zhou, Xue-Quan, Bretin, Ludovic, Zeng, Xiaolong, Husiev, Yurii, Polanco, Ehider A., Zhao, Gangyin, Wijaya, Lukas S., Biver, Tarita, Le Dévédec, Sylvia E., Sun, Wen, Bonnet, Sylvestre
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 12.07.2023
• Subjects: Animals; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; brain; brain neoplasms; Brain Neoplasms - drug therapy; Cell Line, Tumor; Coordination Complexes - chemistry; culture media; diastereomers; glioblastoma; green light; Humans; hydrophilicity; Integrins; irradiation; Mice; nanoparticles; neoplasm cells; Peptides; Peptides, Cyclic; photochemotherapy; phototoxicity; Prodrugs - chemistry; Prodrugs - pharmacology; Prodrugs - therapeutic use; reactive oxygen species; ruthenium; Ruthenium - chemistry; Ruthenium - pharmacology

To investigate the potential of tumor-targeting photoactivated chemotherapy, a chiral ruthenium-based anticancer warhead, Λ/Δ-[Ru­(Ph2phen)2(OH2)2]2+, was conjugated to the RGD-containing Ac-MRGDH-NH2 peptide by direct coordination of the M and H residues to the metal. This design afforded two diast...