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Sheng, Qiran, Neaverson, Joseph C., Mahmoud, Tasnim, Stevenson, Clare E. M., Matthews, Susan E. 
ORCID: https://orcid.org/0000-0001-8821-0851 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 Faculty of Science > School of Biological Sciences Faculty of Science > School of Natural Sciences |
| 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: | |
| Depositing User: | Pure Connector |
| Date Deposited: | 28 Jul 2017 05:06 |
| Last Modified: | 30 Jul 2023 23:17 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/64286 |
| DOI: | 10.1039/C7OB00710H |
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