Scaffold stabilization of a G-triplex and study of its interactions with G-quadruplex targeting ligands

• Published in: Organic & biomolecular chemistry Vol. 17; no. 38; pp. 8726 - 8736
• Main Authors: Bonnat, Laureen, Dautriche, Maelle, Saidi, Taous, Revol-Cavalier, Johana, Dejeu, Jérôme, Defrancq, Eric, Lavergne, Thomas
• Format: Journal Article
• Language: English
• Published: CAMBRIDGE Royal Soc Chemistry 14.10.2019; Royal Society of Chemistry
• Subjects: Binding; Chemical Sciences; Chemistry; Chemistry, Organic; Deoxyribonucleic acid; DNA; DNA - chemistry; G-Quadruplexes; Ligands; Medicinal Chemistry; or physical chemistry; Physical Sciences; Science & Technology; Theoretical and; G-HAIRPIN; PATHWAY; BINDING; INVOLVEMENT
• ISSN: 1477-0520; 1477-0539
• DOI: 10.1039/c9ob01537j

G-triplex nucleic acid structures (G3) have been conjectured to form in vivo but little is known about their physiological functions. The identification of ligands capable of specific binding to G3 structures is therefore highly appealing but remains elusive. Here we report on the assembly of a DNA conjugate which folds into a stable G3 structure. The structural mimic was used to probe the interactions between a G3 ligand and first-in-class G4 ligands, revealing signification binding promiscuity. We have assembled a DNA conjugate which folds into a stable G-triplex structure and used it to demonstrate the binding promiscuity of G-quadruplex targeting ligands.