G-quadruplex binding ligands: from naturally occurring to rationally designed molecules

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-quadruple...

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Bibliographic Details
Published inCurrent pharmaceutical design Vol. 18; no. 14; p. 1948
Main Authors Vy Thi Le, Tuong, Han, Sujin, Chae, Junghyun, Park, Hyun-Ju
Format Journal Article
LanguageEnglish
Published United Arab Emirates 01.05.2012
Subjects
Acridines - pharmacology
Anthraquinones - pharmacology
Berberine - pharmacology
DNA - chemistry
Drug Design
G-Quadruplexes
Humans
Indole Alkaloids - pharmacology
Ligands
Oxazoles - pharmacology
Porphyrins - pharmacology
Quinolines - pharmacology
RNA - chemistry
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Summary: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.
ISSN:1873-4286
DOI:10.2174/138161212799958431