Quadruplex Nucleic Acids As Targets For Medicinal Chemistry

Quadruplex Nucleic Acids As Targets For Medicinal Chemistry

1st Edition - August 25, 2020

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  • Editor: Stephen Neidle
  • eBook ISBN: 9780128210185
  • Hardcover ISBN: 9780128210178

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The realisation that human, animal, viral and bacterial genomes all contain over-representation of higher-order quadruplex structures in regulatory and other pharmacologically-useful regions, has led to a large number of studies aimed at exploiting this findings for therapeutic and diagnostic purposes. Quadruplex-binding small molecules are starting to be evaluated in human clinical trials.

Key Features

  • Provides the authority and expertise of leading contributors from an international board of authors
  • Presents the latest release in the Annual Reports in Medicinal Chemistry series


Undergraduates, graduates, academics and researchers in the field of medicinal chemistry

Table of Contents

  • Part 1. Fundamentals of quadruplexes and their biology

      1. Fundamentals of G-quadruplex biology
      2. F. Brad Johnson

      3. Quadruplex structure and diversity
      4. Fernaldo Richtia Winnerdy and Anh Tuân Phan

        Part 2. Quadruplex targets in human and other organisms

      5. Telomeric quadruplexes as therapeutic targets
      6. Sefan Asamitsu, Norifumi Shioda and Hiroshi Sugiyama

      7. Viral G-quadruplexes: New frontiers in virus pathogenesis and antiviral therapy
      8. Emanuela Ruggiero and Sara N. Richter

      9. Quadruplex detection in human cells
      10. David Monchaud

        Part 3. Discovery and design of quadruplex-binding compounds

      11. An overview of quadruplex ligands: Their common features and chemotype diversity
      12. Valentina Pirota, Michele Stasi, Alessandra Benassi and Filippo Doria

      13. Molecular dynamics simulations of G-quadruplexes: The basic principles and their application to folding and ligand binding
      14. Jiri Sponer, Barira Islam, Petr Stadlbauer and Shozeb Haider

      15. Quadruplex-interacting compounds for regulating the translation of the Epstein–Barr virus nuclear antigen 1 (EBNA1) mRNA: A new strategy to prevent and treat EBV-related cancers
      16. Anton Granzhan, Rodrigo Prado Martins, Robin Fåhraeus, Marc Blondel and Marie-Paule Teulade-Fichou

      17. Click and combinatorial approaches to quadruplex ligand discovery
      18. Jyotirmayee Dash, Puja Saha and Khushnood Fatma

      19. Quadruplex nucleic acids in KRAS targeted-cancer therapy
      20. Luigi E. Xodo

      21. Transcriptional regulation of MYC through G-quadruplex structures
      22. Sumirtha Balaratnam and John S. Schneekloth

      23. KIT promoter: Structure, function and targeting
      24. Silvia Ceschi and Claudia Sissi

      25. Quadruplex targets in neurodegenerative diseases
      26. Janez Plavec

      27. Metal complexes as G-quadruplex binders
      28. Tim Kench and Ramon Vilar

      29. Challenges in developing small-molecule quadruplex therapeutics

    Stephen Neidle

Product details

  • No. of pages: 564
  • Language: English
  • Copyright: © Academic Press 2020
  • Published: August 25, 2020
  • Imprint: Academic Press
  • eBook ISBN: 9780128210185
  • Hardcover ISBN: 9780128210178

About the Serial Editor

Stephen Neidle

Stephen Neidle
Stephen Neidle is an Emeritus Professor of Chemical Biology at University College London, where he has also been the Director of Research in the School of Pharmacy. He has published over 500 primary papers and reviews and is a principal inventor on 14 patent filings. He has also written and edited several books on nucleic acids and anti-cancer drugs.

Affiliations and Expertise

Emeritus Professor of Chemical Biology, The School of Pharmacy, University College London, UK

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