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Article Dans Une Revue Molecules Année : 2023

Novel Synthesis of IMC-48 and Affinity Evaluation with Different i-Motif DNA Sequences

Résumé

During the last decade, the evidence for the biological relevance of i-motif DNA (i-DNA) has been accumulated. However, relatively few molecules were reported to interact with i-DNA, and a controversy concerning their binding mode, affinity, and selectivity persists in the literature. In this context, the cholestane derivative IMC-48 has been reported to modulate bcl-2 gene expression by stabilizing an i-motif structure in its promoter. In the present contribution, we report on a novel, more straightforward, synthesis of IMC-48 requiring fewer steps compared to the previous approach. Furthermore, the interaction of IMC-48 with four different i-motif DNA sequences was thoroughly investigated by bio-layer interferometry (BLI) and circular dichroism (CD) spectroscopy. Surprisingly, our results show that IMC-48 is a very weak ligand of i-DNA as no quantifiable interaction or significant stabilization of i-motif structures could be observed, raising a quest for an alternative mechanism of its biological activity.
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Dates et versions

hal-03933153 , version 2 (10-01-2023)
hal-03933153 , version 1 (09-10-2023)

Identifiants

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Florian Berthiol, Joseph Boissieras, Hugues Bonnet, Marie Pierrot, Christian Philouze, et al.. Novel Synthesis of IMC-48 and Affinity Evaluation with Different i-Motif DNA Sequences. Molecules, 2023, 28 (2), pp.28020682 (13). ⟨10.3390/molecules28020682⟩. ⟨hal-03933153v1⟩
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