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Quadruplex Nucleic Acids As Targets For Medicinal Chemistry. Annual Reports in Medicinal Chemistry Volume 54

  • Book

  • August 2020
  • Elsevier Science and Technology
  • ID: 5007946

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.

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Table of 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 Tu?n 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 F?hraeus, 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