title: Ligand binding to tetra-end-linked (TGGGGT)4 G-quadruplexes: an electrospray mass spectroscopy study.
abstract: The binding properties of a series of known G-quadruplex ligands have been studied by ESI-MS experiments. The tetramolecular (TG(4)T)(4) quadruplex and its analogues I and II blocked, respectively, at the 3' or 5'-end by a tetra-end-linker (TEL) unit were chosen as the ligands targets. The stoichiometries of the obtained complexes as well as the ligand affinity and selectivity to the different quadruplexes were determined to deduce the ligand binding site. The TEL derivatives I and II allowed the probing of the grooves contribution to the binding of ligands to G-quadruplexes, demonstrating that the 3' and 5' quartets are not equivalent binding sites for ligand end-stacking.
authors.affiliation: Dipartimento di Chimica delle Sostanze Naturali, Università degli Studi di Napoli Federico II, Via D. Montesano 49, I-80131 Napoli, Italy.
authors.forename: Jussara
authors.initials: J
authors.lastname: Amato
authors.forename: Giorgia
authors.initials: G
authors.lastname: Oliviero
authors.forename: Nicola
authors.initials: N
authors.lastname: Borbone
authors.forename: Stefano
authors.initials: S
authors.lastname: D'Errico
authors.forename: Gennaro
authors.initials: G
authors.lastname: Piccialli
authors.forename: Patrick
authors.initials: P
authors.lastname: Mailliet
authors.forename: Frédéric
authors.initials: F
authors.lastname: Rosu
authors.forename: Edwin
authors.initials: E
authors.lastname: De Pauw
authors.forename: Valérie
authors.initials: V
authors.lastname: Gabelica
mesh_terms: D001665:Binding Sites; D004214:Distamycins / Q000737:chemistry; D054856:G-Quadruplexes; D008024:Ligands; D008958:Models, Molecular; D009838:Oligodeoxyribonucleotides / Q000737:chemistry*; D010569:Perylene / Q000031:analogs & derivatives / Q000737:chemistry; D010880:Piperidines / Q000737:chemistry; D011166:Porphyrins / Q000737:chemistry; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D004214:Distamycins; D008024:Ligands; C116108:N,N'-bis(2-1(piperidino)-ethyl)-3,4,9,10-perylene-tetracarboxylic diimide; D009838:Oligodeoxyribonucleotides; D010880:Piperidines; D011166:Porphyrins; C021096:tetra(4-N-methylpyridyl)porphine; D010569:Perylene; C030000:stallimycin