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Org Biomol Chem ; 15(27): 5669-5673, 2017 Jul 21.
Artigo em Inglês | MEDLINE | ID: mdl-28567459

RESUMO

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.


Assuntos
DNA/química , Corantes Fluorescentes/química , Substâncias Intercalantes/química , Sítios de Ligação , Ligantes , Estrutura Molecular , Motivos de Nucleotídeos
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