Quadruplex Nucleic Acids As Targets For Medicinal Chemistry

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

F. Brad Johnson

2. Quadruplex structure and diversity

Fernaldo Richtia Winnerdy and Anh Tuân Phan

Part 2. Quadruplex targets in human and other organisms

3. Telomeric quadruplexes as therapeutic targets

Sefan Asamitsu, Norifumi Shioda and Hiroshi Sugiyama

4. Viral G-quadruplexes: New frontiers in virus pathogenesis and antiviral therapy

Emanuela Ruggiero and Sara N. Richter

5. Quadruplex detection in human cells

David Monchaud

Part 3. Discovery and design of quadruplex-binding compounds

6. An overview of quadruplex ligands: Their common features and chemotype diversity

Valentina Pirota, Michele Stasi, Alessandra Benassi and Filippo Doria

7. Molecular dynamics simulations of G-quadruplexes: The basic principles and their application to folding and ligand binding

Jiri Sponer, Barira Islam, Petr Stadlbauer and Shozeb Haider

8. 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

Anton Granzhan, Rodrigo Prado Martins, Robin Fåhraeus, Marc Blondel and Marie-Paule Teulade-Fichou

9. Click and combinatorial approaches to quadruplex ligand discovery

Jyotirmayee Dash, Puja Saha and Khushnood Fatma

10. Quadruplex nucleic acids in KRAS targeted-cancer therapy

Luigi E. Xodo

11. Transcriptional regulation of MYC through G-quadruplex structures

Sumirtha Balaratnam and John S. Schneekloth

12. KIT promoter: Structure, function and targeting

Silvia Ceschi and Claudia Sissi

13. Quadruplex targets in neurodegenerative diseases

Janez Plavec

14. Metal complexes as G-quadruplex binders

Tim Kench and Ramon Vilar

15. Challenges in developing small-molecule quadruplex therapeutics