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Ruthenium-peptide conjugates for targeted phototherapy

As leading cause of death worldwide, cancer is responsible for nearly 10 million deaths in 2020 according to World Health Organization (WHO). Cisplatin and its derivatives are commonly used chemotherapy agents for current cancer treatment in the clinics.

L. Zhang
04 July 2023
Thesis in Leiden Repository

While such metallodrugs are urgent to be improved because they are often accompanied by severe side effects to the patients. Alternatively, ruthenium-based complex are considered as more promising candidates due to their appealing photochemistry and photophysical properties. These properties offer possibility to activate such complex by external light, which realizes a better partial targeting to tumor region and thus reduces the side effect of the metallodrugs. To further optimize the tumor selectivity of ruthenium complexes, in this thesis, a series of ruthenium(Ⅱ) polypyridine-peptide conjugates were synthesized differential in polypyridine ligand, peptide sequence, and/or chirality. Their structure, photochemistry, in vitro cellular behaviors, and in vivo antitumor efficiency, were widely studied and compared. My study confirmed that the conjugation of peptides with ruthenium complexes is one of the most promising tools for improving their potential as clinical drugs, which provides a strong basis for the design and application of more ruthenium-peptide candidates for active tumor targeting in the future.

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