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To demonstrate the versatility of this pro\u2010chelator for the preparation of radiolabeled hybrid compounds containing two different biological targeting moieties, an antitumor agent (e.g., a DNA\u2010intercalating agent) and an estrogen receptor (ER) ligand (e.g., LXXLL\u2010based peptide) were regiospecifically conjugated to the DOTA derivative. The bifunctional probe was radiolabeled with the auger electron emitter indium\u2010111, and the resulting radioconjugate was demonstrated to induce DNA damage in\u2005vitro, which, along with the nuclear internalization exhibited in breast cancer cells, might enhance its therapeutic activity. 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