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C2TN

ACRIDINE ORANGE DERIVATIVES FOR DNA-TARGETING

G1 4

Applications using radioisotopes and radiopharmaceuticals are of major importance for cancer medicine and paved the way for the development of targeted radionuclide therapies and more advanced diagnostic techniques. Within targeted radionuclide therapies, Auger-emitting radiopharmaceuticals are considered best suited for the eradication of disseminated cancer metastases with minimization of deleterious effect to non-target surrounding tissues. To tackle this goal, we have been involved in the study of 125I- and 99mTc-containing acridine orange (AO) derivatives as potential Auger-emitting radiopharmaceuticals. In collaboration with the group of Carla Cruz (CICS-UBI, Covilhã), we have recently demonstrated that some of these AO derivatives are potent binders of G-quadruplex (G4) structures formed within the nuclease hypersensitive element of the KRAS promoter region. This finding might have great relevance for the design of innovative Auger-emitting radiopharmaceuticals targeted at KRAS, as KRAS is often found mutated in a variety of highly lethal cancers.