Main description:

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.

Contents:

Part 1. Fundamentals of quadruplexes and their biology

Fundamentals of G-quadruplex biology
F. Brad Johnson

Quadruplex structure and diversity
Fernaldo Richtia Winnerdy and Anh Tuan Phan

Part 2. Quadruplex targets in human and other organisms

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

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

Quadruplex detection in human cells
David Monchaud

Part 3. Discovery and design of quadruplex-binding compounds

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

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

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 Fahraeus, Marc Blondel and Marie-Paule Teulade-Fichou

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

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

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

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

Quadruplex targets in neurodegenerative diseases
Janez Plavec

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

Challenges in developing small-molecule quadruplex therapeutics

Stephen Neidle