title: G-quadruplex recognition by quinacridines: a SAR, NMR, and biological study.
abstract: The synthesis of a novel group of quinacridine-based ligands (MMQs) is described along with an evaluation of their G-quadruplex binding properties. A set of biophysical assays was applied to characterize their interaction with DNA quadruplexes: FRET-melting experiments and equilibrium microdialysis were used to evaluate their quadruplex affinity and their ability to discriminate quadruplexes across a broad panel of DNA structures. All data collected support the proposed model of interaction of these compounds with G-quadruplexes, which is furthermore confirmed by a solution structure determined by 2D NMR experiments. Finally, the activity of the MMQ series against tumor cell growth is reported, and the data support the potential of quadruplex-interactive compounds for use in anticancer approaches.
authors: Laboratoire de Chimie des Interactions Moléculaires, CNRS UPR 285, Collège de France, 11, place Marcellin Berthelot, 75005 Paris, France.
authors: Candide
authors: C
authors: Hounsou
authors: Lionel
authors: L
authors: Guittat
authors: David
authors: D
authors: Monchaud
authors: Muriel
authors: M
authors: Jourdan
authors: Nicolas
authors: N
authors: Saettel
authors: Jean-Louis
authors: JL
authors: Mergny
authors: Marie-Paule
authors: MP
authors: Teulade-Fichou
mesh_terms: D000166:Acridines / Q000737:chemistry*; D031541:Fluorescence Resonance Energy Transfer; D009682:Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship
chemical_list: D000166:Acridines