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

Sheng, Qiran, Neaverson, Joseph C., Mahmoud, Tasnim, Stevenson, Clare E. M., Matthews, Susan E. and Waller, Zoë A. E. (2017) Identification of new DNA i-motif binding ligands through a fluorescent intercalator displacement assay. Organic & Biomolecular Chemistry, 15 (27). pp. 5669-5673. ISSN 1477-0520

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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.

Item Type: Article
Faculty \ School: Faculty of Science > School of Pharmacy
Faculty of Science > School of Biological Sciences
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Depositing User: Pure Connector
Date Deposited: 28 Jul 2017 05:06
Last Modified: 31 Oct 2019 15:11
URI: https://ueaeprints.uea.ac.uk/id/eprint/64286
DOI: 10.1039/C7OB00710H

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