Therapeutic Applications of Quadruplex Nucleic Acids


  • Stephen Neidle, The School of Pharmacy, University College London, UK

The study of G-quadruplexes has emerged in recent years as an important focus of research in nucleic acids. This is now a rapidly growing area, not least because of its potential as a novel approach to cancer therapeutics, and there is much current activity on the design of quadruplex-selective small-molecule ligands and the study of their cellular effects. This timely publication gives a uniquely integrated view of quadruplex nucleic acids that will be a major resource in future drug-discovery strategies.

Therapeutic Applications of Quadruplex Nucleic Acids provides a single comprehensive survey that describes and assesses recent advances in quadruplex therapeutics and targeting strategies. It also covers the underlying fundamentals of such topics as quadruplex structure, small-molecule recognition, biological roles of genomic quadruplexes, and quadruplex informatics.

Written by a world leader in this field, this book is a vital resource for researchers in medicinal chemistry, chemical biology, structural biology, drug discovery, and pharmacology in cancer and other therapeutic areas, as well as for chemists and biologists working on nucleic acids, and will be useful for both active researchers and students in these areas.

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Biochemists, chemists, professional researchers in laboratories in academic, government and corporate environments studying translational science, medicine and pharmacology, as well as, advanced undergraduate students, graduate students and medical students.


Book information

  • Published: September 2011
  • ISBN: 978-0-12-375138-6

Table of Contents

  1. Intro - history and milestones
  2. Fundamentals of DNA and RNA quadruplex structure and stability
  3. Quadruplexes as therapeutic targets for telomeres and relationship to telomerase and telomere maintenance
  4. Genomic DNA and RNA quadruplexes - involvement in gene expression and potential as therapeutic agents
  5. Quadruplex targets and human disease - applicability in cancer and infectious disease, including oncogene targets such as c-myc and c-kit
  6. Quadruplex ligands - chemistry and design - selectivity and assays
  7. Quadruplex ligands - basic biology and assays indirect and direct
  8. Quadruplex ligands - pharmacology and druggability, ligands in clinical trial and pre-clinical trial development
  9. Synthetic quadruplexes and drugs - therapeutic aptamers, including thrombin, STAT3 binding, nucleolin binding
  10. Future directions and conclusions