Nanomolar Selective G Quadruplex Ligands from One Pot Thermodynamic and Structural Studies of Azacyanines

Date

2008-11-15

Author

Engelhart, Aaron
Persil Çetinkol, Özgül
Nanjunda, Rupesh
Wılson, Davıd
Hud, Nıcholas

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The observation that G-quadruplex structures exist in nucleic acid sequences associated with cancers has generated substantial interest in G quadruplexes as potential antineoplastics. The G quadruplex, with planar G tetrads, is an appealing nucleic acid drug target, as the G tetrad is structurally distinct from the Watson-Crick base pair. 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 a novel, high-affinity, high-selectivity scaffold for G-quadruplex ligands: the azacyanines. We present data on the G-quadruplex and Watson-Crick dsDNA binding affinity of these ligands. 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 solution.

URI

https://hdl.handle.net/11511/79644

Conference Name

Southeast Regional Meeting of the ACS (2008)

Collections

Department of Chemistry, Conference / Seminar

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Citation Formats

A. Engelhart, Ö. Persil Çetinkol, R. Nanjunda, D. Wılson, and N. Hud, “Nanomolar Selective G Quadruplex Ligands from One Pot Thermodynamic and Structural Studies of Azacyanines,” presented at the Southeast Regional Meeting of the ACS (2008), 2008, Accessed: 00, 2021. [Online]. Available: https://hdl.handle.net/11511/79644.