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2022-07-26

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cc-by (c) Mazzini, Stefania et al., 2022
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/190045

Exploring the Interaction of G-quadruplex Binders with a (3 + 1) Hybrid G-quadruplex Forming Sequence within the PARP1 Gene Promoter Region

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Abstract

The enzyme PARP1 is an attractive target for cancer therapy, as it is involved in DNA repair processes. Several PARP1 inhibitors have been approved for clinical treatments. However, the rapid outbreak of resistance is seriously threatening the efficacy of these compounds, and alternative strategies are required to selectively regulate PARP1 activity. A noncanonical G-quadruplex-forming sequence within the PARP1 promoter was recently identified. In this study, we explore the interaction of known G-quadruplex binders with the G-quadruplex structure found in the PARP gene promoter region. The results obtained by NMR, CD, and fluorescence titration, also confirmed by molecular modeling studies, demonstrate a variety of different binding modes with small stabilization of the G-quadruplex sequence located at the PARP1 promoter. Surprisingly, only pyridostatin produces a strong stabilization of the G-quadruplex-forming sequence. This evidence makes the identification of a proper (3+1) stabilizing ligand a challenging goal for further investigation.

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Models moleculars, ADN, G-estructures

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Molecular models, DNA, G-structures

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Articles publicats en revistes (Enginyeria Química i Química Analítica)

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MAZZINI, Stefania, et al. Exploring the Interaction of G-quadruplex Binders with a (3 + 1) Hybrid G-quadruplex Forming Sequence within the PARP1 Gene Promoter Region. Molecules. 2022. Vol. 27, num. 15, pags. 4792. ISSN 1420-3049. [consulted: 14 of August of 2026]. Available at: https://hdl.handle.net/2445/190045

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