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We report here a supramolecular strategy to assemble a cyclodextrin-functionalized anticancer Ru(II) complex with an adamantane-appended tumor-targeting peptide into discrete and stable phosphorescent nanostructures that can induce cell death in integrin αvβ3-rich tumor cells with high selectivity. This strategy presents new opportunities for the construction of tumor-targeting metallo-anticancer therapeutics.

Graphical abstract: Tumor-targeted supramolecular nanoparticles self-assembled from a ruthenium-β-cyclodextrin complex and an adamantane-functionalized peptide

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