caa a22 4500 605507457 CHVBK 20210128100632.0 cr unu---uuuuu 210128e20150601xx s 000 0 eng 10.1007/s00775-015-1260-8 doi (NATIONALLICENCE)springer-10.1007/s00775-015-1260-8 The nickel(II) complex of guanidinium phenyl porphyrin, a specific G-quadruplex ligand, targets telomeres and leads to POT1 mislocalization in culture cells [Elektronische Daten] [Laurent Sabater, Marie-Laure Nicolau-Travers, Aurore De Rache, Enora Prado, Jérôme Dejeu, Oriane Bombarde, Joris Lacroix, Patrick Calsou, Eric Defrancq, Jean-Louis Mergny, Dennis Gomez, Geneviève Pratviel] With the aim of finding selective and biologically active G-quadruplex ligands, modified porphyrin with bulky cationic substituents, meso-5,10,15,20-tetrakis(4-guanidinophenyl)porphyrin tetrahydrochloride, referred to as guanidinium phenyl porphyrin, was prepared. The corresponding nickel(II) and cobalt(III) metallated porphyrins were also synthesized. Interaction with quadruplexes was examined by means of fluorescence resonance energy transfer melting and surface plasmon resonance-based assays: the three compounds proved to bind to G-quadruplex DNA in a similar and highly selective way. Guanidinium phenyl porphyrin and its nickel(II) metallated derivative exhibit moderate cytotoxicity toward cells in culture. Strikingly, the nickel porphyrin derivative was able to displace hPOT1 shelterin protein from telomeres in human cells. Graphical Abstract: Nickel(II) guanidinium phenyl porphyrin, a cationic bulky porphyrin is a powerful specific G-quadruplex DNA ligand. It enters the cells and induces shelterin modification. SBIC, 2015 G4 ligand nationallicence Telomere nationallicence Porphyrin nationallicence G-quadruplex nationallicence POT1 nationallicence Sabater Laurent Centre National de la Recherche Scientifique, Laboratoire de Chimie de Coordination, 205 Route de Narbonne, 31077, Toulouse, France aut Nicolau-Travers Marie-Laure Centre National de la Recherche Scientifique, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France aut De Rache Aurore Laboratoire ARNA, Université de Bordeaux, 33000, Bordeaux, France aut Prado Enora Université Grenoble Alpes, DCM, 38000, Grenoble, France aut Dejeu Jérôme Université Grenoble Alpes, DCM, 38000, Grenoble, France aut Bombarde Oriane Centre National de la Recherche Scientifique, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France aut Lacroix Joris Centre National de la Recherche Scientifique, Laboratoire de Chimie de Coordination, 205 Route de Narbonne, 31077, Toulouse, France aut Calsou Patrick Centre National de la Recherche Scientifique, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France aut Defrancq Eric Université Grenoble Alpes, DCM, 38000, Grenoble, France aut Mergny Jean-Louis Laboratoire ARNA, Université de Bordeaux, 33000, Bordeaux, France aut Gomez Dennis Centre National de la Recherche Scientifique, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France aut Pratviel Geneviève Centre National de la Recherche Scientifique, Laboratoire de Chimie de Coordination, 205 Route de Narbonne, 31077, Toulouse, France aut JBIC Journal of Biological Inorganic Chemistry Springer Berlin Heidelberg 20/4(2015-06-01), 729-738 0949-8257 20:4<729 2015 20 775 https://doi.org/10.1007/s00775-015-1260-8 text/html Onlinezugriff via DOI BK010053 XK010053 XK010000 Metadata rights reserved Springer special CC-BY-NC licence nationallicence 1 research-article jats NATIONALLICENCE NATIONALLICENCE NL-springer NATIONALLICENCE 856 40 https://doi.org/10.1007/s00775-015-1260-8 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Sabater Laurent Centre National de la Recherche Scientifique, Laboratoire de Chimie de Coordination, 205 Route de Narbonne, 31077, Toulouse, France aut NATIONALLICENCE 700 1- Nicolau-Travers Marie-Laure Centre National de la Recherche Scientifique, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France aut NATIONALLICENCE 700 1- De Rache Aurore Laboratoire ARNA, Université de Bordeaux, 33000, Bordeaux, France aut NATIONALLICENCE 700 1- Prado Enora Université Grenoble Alpes, DCM, 38000, Grenoble, France aut NATIONALLICENCE 700 1- Dejeu Jérôme Université Grenoble Alpes, DCM, 38000, Grenoble, France aut NATIONALLICENCE 700 1- Bombarde Oriane Centre National de la Recherche Scientifique, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France aut NATIONALLICENCE 700 1- Lacroix Joris Centre National de la Recherche Scientifique, Laboratoire de Chimie de Coordination, 205 Route de Narbonne, 31077, Toulouse, France aut NATIONALLICENCE 700 1- Calsou Patrick Centre National de la Recherche Scientifique, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France aut NATIONALLICENCE 700 1- Defrancq Eric Université Grenoble Alpes, DCM, 38000, Grenoble, France aut NATIONALLICENCE 700 1- Mergny Jean-Louis Laboratoire ARNA, Université de Bordeaux, 33000, Bordeaux, France aut NATIONALLICENCE 700 1- Gomez Dennis Centre National de la Recherche Scientifique, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France aut NATIONALLICENCE 700 1- Pratviel Geneviève Centre National de la Recherche Scientifique, Laboratoire de Chimie de Coordination, 205 Route de Narbonne, 31077, Toulouse, France aut NATIONALLICENCE 773 0- JBIC Journal of Biological Inorganic Chemistry Springer Berlin Heidelberg 20/4(2015-06-01), 729-738 0949-8257 20:4<729 2015 20 775