G-Quadruplex Binding Ligands: from Naturally Occurring to Rationally Designed Molecules

Title:G-Quadruplex Binding Ligands: from Naturally Occurring to Rationally Designed Molecules

Volume: 18 Issue: 14

Author(s): Tuong Vy Thi Le, Sujin Han, Junghyun Chae and Hyun-Ju Park

Affiliation:

Keywords: DNA G-quadruplex, RNA G-quadruplex, telomere, oncogene promoter G- quadruplex, telomeric RNA, guanine-rich, polymorphism, X-ray crystallographic, aromatic rings, electron-deficient

Abstract: Guanine-rich nucleic acid sequences are known to form G-quadruplex - four-stranded DNA or RNA structures stabilized by an array of Hoogsteen hydrogen bonds. G-quadruplex structures are involved in the modulation of gene expression at the transcription and translation levels. Accordingly, G-quadruplexes are considered as novel therapeutic targets for anticancer drug development. In this review, the authors provide a brief, up-to-date summary of G-quadruplex binding ligands, including naturally occurring molecules, synthetic compounds, and molecules identified by computational database screening. The key structural motifs of G-quadruplex binding ligands, that is, an aromatic core and basic side chains, are addressed in the context of how these molecules interact with G-quadruplex. A better understanding of these interactions would facilitate the rational design of ligands selective for DNA or RNA G-quadruplex.

Cite this article as:

Vy Thi Le Tuong, Han Sujin, Chae Junghyun and Park Hyun-Ju, G-Quadruplex Binding Ligands: from Naturally Occurring to Rationally Designed Molecules, Current Pharmaceutical Design 2012; 18 (14) . https://dx.doi.org/10.2174/138161212799958431