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

Title	Cyclic Ruthenium-Peptide Conjugates as Integrin-Targeting Phototherapeutic Prodrugs for the Treatment of Brain Tumours
Authors	Liyan Zhang, Peiyuan Wang, Xue-Quan Zhou, Ludovic Bretin, Xiaolong Zeng, Yurii Husiev, Ehider A. Polanco, Gangyin Zhao, Lukas S. Wijaya, Tarita Biver, Sylvia E. Le Dévédec, Wen Sun, Sylvestre Bonnet
Magazine	Journal of the American Chemical Society
Date	06/28/2023
DOI	10.1021/jacs.3c04855
Introduction	This study evaluates tumour-targeting photoactivated chemotherapy using a chiral ruthenium-based anticancer agent conjugated to an RGD-containing peptide. The cyclic metallopeptides Λ-[1]Cl2 and Δ-[1]Cl2 exhibit triple action by preventing metal coordination with biomolecules, forming amphiphilic nanoparticles, and targeting integrins. Phototoxicity was confirmed in 2D cancer cell monolayers and 3D tumour spheroids, with significant tumouricidal effects observed under green light irradiation in vivo. These results highlight the promise of integrin-targeted ruthenium-based compounds for brain cancer treatment without systemic toxicity.
Quote	Liyan Zhang, Peiyuan Wang and Xue-Quan Zhou et al. Cyclic Ruthenium-Peptide Conjugates as Integrin-Targeting Phototherapeutic Prodrugs for the Treatment of Brain Tumours. J. Am. Chem. Soc. 2023. Vol. 145(27):14963-14980. DOI: 10.1021/jacs.3c04855
Element	Ruthenium (Ru)
Materials	Chemical Compounds
Industry	Pharmaceutical Industry

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