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G-quadruplex ligands exhibit differential G-tetrad selectivity.


Type

Article

Change log

Authors

Le, DD 
Chan, LKM 
Balasubramanian, Shankar  ORCID logo  https://orcid.org/0000-0002-0281-5815

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

Volume Title

51

Publisher

Royal Society of Chemistry (RSC)
Sponsorship
Biotechnology and Biological Sciences Research Council (BB/K018043/1)
Engineering and Physical Sciences Research Council (EP/K039520/1)
Cancer Research UK (18618)
Cancer Research Uk (None)
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.