Issue 14, 2021

Phenoxazine pseudonucleotides in DNA i-motifs allow precise profiling of small molecule binders by fluorescence monitoring

Abstract

The lack of high throughput screening (HTS) techniques for small molecules that stabilize DNA iMs limits their development as perspective drug candidates. Here we showed that fluorescence monitoring for probing the effects of ligands on the iM stability using the FAM–BHQ1 pair provides incorrect results due to additional dye-related interactions. We developed an alternative system with fluorescent phenoxazine pseudonucleotides in loops that do not alter iM unfolding. At the same time, the fluorescence of phenoxazine residues is sensitive to iM unfolding that enables accurate evaluation of ligand-induced changes of iM stability. Our results provide the basis for new approaches for HTS of iM ligands.

Graphical abstract: Phenoxazine pseudonucleotides in DNA i-motifs allow precise profiling of small molecule binders by fluorescence monitoring

Supplementary files

Article information

Article type
Communication
Submitted
16 abr 2021
Accepted
31 mai 2021
First published
31 mai 2021

Analyst, 2021,146, 4436-4440

Phenoxazine pseudonucleotides in DNA i-motifs allow precise profiling of small molecule binders by fluorescence monitoring

V. B. Tsvetkov, A. V. Turaev, N. A. Petrunina, D. M. Melnik, Y. M. Khodarovich, G. E. Pozmogova, T. S. Zatsepin, A. M. Varizhuk and A. V. Aralov, Analyst, 2021, 146, 4436 DOI: 10.1039/D1AN00660F

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