Book of Abstracts: Albany 2009

category image Albany 2009
Conversation 16
June 16-20 2009
© Adenine Press (2008)

Selective, High-affinity, Synthetically Accessible Ligands for G-quadruplex DNA: Thermodynamic and Structural Studies of Azacyanines

G-quadruplex ligands have attracted substantial interest recently as potential antineoplastics. The G quadruplex is an appealing nucleic acid drug target, as the G tetrad is structurally distinct from the Watson-Crick base pair. Additionally, the backbone geometries and groove widths differ between G quadruplexes and dsDNA. High-affinity G-quadruplex ligands have begun to show medicinal promise, although the connection between G-quadruplex binding and in vivo activity might not always be obvious. Here, we report novel, high-affinity, high-selectivity G-quadruplex ligands: the azacyanines. We present data comparing the G-quadruplex and Watson-Crick dsDNA binding affinities of these molecules (1). Additionally, we present data related to the binding site for these ligands on the G quadruplex formed by the human telomeric DNA repeat in potassium containing solution.

References and Footnotes
  1. Çetinkol ÖP, Engelhart AE, Nanjunda RK, Wilson WD, Hud NV. ChemBioChem 9:1889?1892 (2008).

Aaron E. Engelhart
Özgül Persil Çetinkol
Rupesh K. Nanjunda
W. David Wilson
Nicholas V. Hud.

Department of Chemistry and Biochemistry
Georgia Institute of Technology
315 Ferst Dr.
Atlanta, GA 30332

Phone: 404-385-1166
Fax: 404-894-7452
email Aaron Engelhart