Submicromolar, Selective G-Quadruplex Ligands from One Pot: Thermodynamic and Structural Studies of Human Telomeric DNA Binding by Azacyanines

• Published in: Chembiochem : a European journal of chemical biology Vol. 9; no. 12; pp. 1889 - 1892
• Main Authors: Persil Çetinkol, Özgül, Engelhart, Aaron E, Nanjunda, Rupesh K, Wilson, W. David, Hud, Nicholas V
• Format: Journal Article
• Language: English
• Published: Weinheim Wiley-VCH Verlag 11-08-2008; WILEY-VCH Verlag; WILEY‐VCH Verlag
• Subjects: Animals; Aza Compounds - chemistry; Aza Compounds - metabolism; Base Sequence; cancer; Cattle; DNA - chemistry; DNA - genetics; DNA - metabolism; DNA structures; drug design; G-Quadruplexes; Humans; Ligands; quadruplexes; Spectrometry, Fluorescence; Substrate Specificity; Telomere - genetics; telomeres; Thermodynamics
• ISSN: 1439-4227; 1439-7633
• DOI: 10.1002/cbic.200800234

Bound to work: A molecular architecture with a shape that is slightly larger than a Watson–Crick base pair was investigated as a potential G‐quadruplex ligand. Azacyanines, which possess this architecture, were found to bind on the end of the quadruplex stack (as shown in the figure) and to exhibit high selectivity over duplex binding. The chemical properties, ease of synthesis, and great potential for modification make the azacyanines and their analogues attractive for development as G‐quadruplex ligands in drug development.