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.; Waller, Zoë A. E.

doi:10.1039/C7OB00710H

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

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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
Uncontrolled Keywords:	sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being
Faculty \ School:	Faculty of Science > School of Pharmacy (former - to 2024) Faculty of Science > School of Biological Sciences Faculty of Science > School of Natural Sciences (former - to 2024)
UEA Research Groups:	Faculty of Science > Research Groups > Medicinal Chemistry (former - to 2017) Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021)
Related URLs:	http://pubs.rsc.org/en/content/articleht...
Depositing User:	Pure Connector
Date Deposited:	28 Jul 2017 05:06
Last Modified:	19 Oct 2025 23:48
URI:	https://ueaeprints.uea.ac.uk/id/eprint/64286
DOI:	10.1039/C7OB00710H

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