G-Quadruplexes and Their Ligands: Biophysical Methods to Unravel G-Quadruplex/Ligand Interactions

Progress in the design of G-quadruplex (G4) binding ligands relies on the availability of approaches that assess the binding mode and nature of the interactions between G4 forming sequences and their putative ligands. The experimental approaches used to characterize G4/ligand interactions can be cat...

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Published inPharmaceuticals (Basel, Switzerland) Vol. 14; no. 8; p. 769
Main Authors Santos, Tiago, Salgado, Gilmar F, Cabrita, Eurico J, Cruz, Carla
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 05.08.2021
MDPI
Subjects
Algorithms
Bacteria
biophysical methods
Cancer
DNA damage
G-quadruplex
Genomes
Ligands
molecular interactions
Neurological disorders
Physiology
R&D
Research & development
Research methodology
Review
Severe acute respiratory syndrome coronavirus 2
ligands
biophysical methods
molecular interactions
G-quadruplex
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Summary:Progress in the design of G-quadruplex (G4) binding ligands relies on the availability of approaches that assess the binding mode and nature of the interactions between G4 forming sequences and their putative ligands. The experimental approaches used to characterize G4/ligand interactions can be categorized into structure-based methods (circular dichroism (CD), nuclear magnetic resonance (NMR) spectroscopy and X-ray crystallography), affinity and apparent affinity-based methods (surface plasmon resonance (SPR), isothermal titration calorimetry (ITC) and mass spectrometry (MS)), and high-throughput methods (fluorescence resonance energy transfer (FRET)-melting, G4-fluorescent intercalator displacement assay (G4-FID), affinity chromatography and microarrays. Each method has unique advantages and drawbacks, which makes it essential to select the ideal strategies for the biological question being addressed. The structural- and affinity and apparent affinity-based methods are in several cases complex and/or time-consuming and can be combined with fast and cheap high-throughput approaches to improve the design and development of new potential G4 ligands. In recent years, the joint use of these techniques permitted the discovery of a huge number of G4 ligands investigated for diagnostic and therapeutic purposes. Overall, this review article highlights in detail the most commonly used approaches to characterize the G4/ligand interactions, as well as the applications and types of information that can be obtained from the use of each technique.
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ISSN:1424-8247
1424-8247
DOI:10.3390/ph14080769