Sequence, Stability, and Structure of G‐Quadruplexes and Their Interactions with Drugs

Yuwei Chen1, Danzhou Yang2

1 Department of Chemistry and Biochemistry, The University of Arizona, Tucson, Arizona, 2 Arizona Cancer Center, Tucson, Arizona
Publication Name:  Current Protocols in Nucleic Acid Chemistry
Unit Number:  Unit 17.5
DOI:  10.1002/0471142700.nc1705s50
Online Posting Date:  September, 2012
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Although DNA is most widely known for its ability to store and pass along genetic information, the discovery of G‐quadruplex structures has illuminated a new role for DNA in biology. DNA G‐quadruplexes are four‐stranded globular nucleic acid secondary structures formed in specific G‐rich sequences with biological significance, such as human telomeres and oncogene promoters. This review focuses on the unimolecular DNA G‐quadruplexes, which can readily form in solution under physiological conditions and are considered to be the most biologically relevant. Available structural data show a great conformational diversity of unimolecular G‐quadruplexes, which are amenable to small‐molecule drug targeting. The relationships between sequence, structure, and stability of unimolecular DNA G‐quadruplexes, as well as the recent progress on interactions with small‐molecule compounds and insights into rational design of G‐quadruplex‐interactive molecules, will be discussed. Curr. Protoc. Nucleic Acid Chem. 50:17.5.1‐17.5.17. © 2012 by John Wiley & Sons, Inc.

Keywords: G‐quadruplexes; oncogene promoters; human telomeres; small‐molecule interactions; rational drug design

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Table of Contents

  • Introduction
  • DNA G‐Quadruplex Folds
  • Interactions of G‐Quadruplexes with Small Molecules
  • Conclusions and Future Direction
  • Acknowledgments
  • Literature Cited
  • Figures
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Literature Cited

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