Issue 27, 2017

Identification of new DNA i-motif binding ligands through a fluorescent intercalator displacement assay

Abstract

i-Motifs are quadruplex DNA structures formed from sequences rich in cytosine and held together by intercalated, hemi-protonated cytosine–cytosine base pairs. These sequences are prevalent in gene promoter regions and may play a role in gene transcription. Targeting these structures with ligands could provide a novel way to target genetic disease but there are very few ligands which have been shown to interact with i-motif DNA. Fluorescent intercalator displacement (FID) assays are a simple way to screen ligands against DNA secondary structures. Here we characterise how thiazole orange interacts with i-motif DNA and assess its ability for use in a FID assay. Additionally, we report FID-based ligand screening using thiazole orange against the i-motif forming sequence from the human telomere to reveal new i-motif binding compounds which have the potential for further development.

Graphical abstract: Identification of new DNA i-motif binding ligands through a fluorescent intercalator displacement assay

Supplementary files

Article information

Article type
Communication
Submitted
22 mrt 2017
Accepted
22 mei 2017
First published
01 jun 2017
This article is Open Access
Creative Commons BY license

Org. Biomol. Chem., 2017,15, 5669-5673

Identification of new DNA i-motif binding ligands through a fluorescent intercalator displacement assay

Q. Sheng, J. C. Neaverson, T. Mahmoud, C. E. M. Stevenson, S. E. Matthews and Z. A. E. Waller, Org. Biomol. Chem., 2017, 15, 5669 DOI: 10.1039/C7OB00710H

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