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Subcellular Duplex DNA and G‐Quadruplex Interaction Profiling of a Hexagonal PtII Metallacycle
Authors:Olaya Domarco,Claudia Kieler,Christine Pirker,Carina Dinhof,Bernhard Englinger,Johannes M. Reisecker,Gerald Timelthaler,Marcos D. Garcí  a,Carlos Peinador,Bernhard K. Keppler,Walter Berger,Alessio Terenzi
Abstract:Metal‐driven self‐assembly afforded a multitude of fascinating supramolecular coordination complexes (SCCs) with applications as catalysts, host–guest, and stimuli‐responsive systems. However, the interest in the biological applications of SCCs is only starting to emerge and thorough characterization of their behavior in biological milieus is still lacking. Herein, we report on the synthesis and detailed in‐cell tracking of a Pt2L2 metallacycle. We show that our hexagonal supramolecule accumulates in cancer cell nuclei, exerting a distinctive blue fluorescence staining of chromatin resistant to UV photobleaching selectively in nucleolar G4‐rich regions. SCC co‐localizes with epitopes of the quadruplex‐specific antibody BG4 and replaces other well‐known G4 stabilizers. Moreover, the photophysical changes accompanying the metallacycle binding to G4s in solution (fluorescence quenching, absorption enhancement) also take place intracellularly, allowing its subcellular interaction tracking.
Keywords:G-Quadruplexe  Metallacyclen  Platin  SCC  Subzellulä  re Lokalisierung
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