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Quadruplex Nucleic Acids As Targets For Medicinal Chemistry

Contains contributions from the best scientists in medicinal chemistry who present the latest developments in the field

Stephen Neidle (Series edited by)

9780128210178, Elsevier Science

Hardback, published 25 August 2020

564 pages
22.9 x 15.1 x 3.2 cm, 1.04 kg

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.

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

Subject Areas: Chemistry [PN], Pharmacology [MMG]

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