G-quadruplex ligands exhibit differential G-tetrad selectivity.
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Authors
Le, DD
Chan, LKM
Abstract
A rapid and simple equilibrium-binding assay mediated by ligand-induced fluorescence quenching of fluorophore-labelled G-quadruplex (G4) structures enabled quantitative interrogation of mutually exclusive ligand binding interactions at opposed G-tetrads. This technique revealed that the ligands TmPyP4, PhenDC3, and PDS have differential chemotype-specific binding preferences for individual G-tetrads of a model genomic G4 structure.
Description
Keywords
Fluorescence, Fluorescent Dyes, G-Quadruplexes, Humans, Ligands, Molecular Structure, Substrate Specificity
Journal Title
Chem Commun (Camb)
Conference Name
Journal ISSN
1359-7345
1364-548X
1364-548X
Volume Title
51
Publisher
Royal Society of Chemistry (RSC)
Publisher DOI
Sponsorship
Biotechnology and Biological Sciences Research Council (BB/K018043/1)
Engineering and Physical Sciences Research Council (EP/K039520/1)
Engineering and Physical Sciences Research Council (EP/K039520/1)
This work was supported by the following grants: Cancer
Research UK Programme, BBSRC BB/K018043/1 and EPSRC EP/
K039520/1. We thank Dr Chris Lowe for his constructive comments
and for proofreading the manuscript.