Complex Biophysical and Computational Analyses of GQuadruplex Ligands: The Porphyrin Stacks Back
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Date
2024-09-18
Authors
Satta, Giuseppe
Trajkovski, Marko
Cantara, Alessio
Mura, Monica
Meloni, Claudia
Olla, Giulia
Dobrovolná, Michaela
Pisano, Luisa
Gaspa, Silvia
Salis, Andrea
ORCID
0000-0003-2837-4226Advisor
Referee
Mark
Journal Title
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Volume Title
Publisher
Wiley-VCH
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Abstract
G-quadruplexes (G4 s), as non-canonical DNA structures, attracta great deal of research interest in the molecular biology as wellas in the material science fields. The use of small molecules asligands for G-quadruplexes has emerged as a tool to regulategene expression and telomeres maintenance. Meso-tetrakis-(N-methyl-4-pyridyl) porphyrin (TMPyP4) was shown as one of thefirst ligands for G-quadruplexes and it is still widely used. Wereport an investigation comprising molecular docking anddynamics, synthesis and multiple spectroscopic and spectro-metric determinations on simple cationic porphyrins and theirinteraction with different DNA sequences. This study enabledthe synthesis of tetracationic porphyrin derivatives that ex-hibited binding and stabilizing capacity against G-quadruplexstructures; the detailed characterization has shown that thepresence of amide groups at the periphery improves selectivityfor parallel G4 s binding over other structures. Taking intoaccount the ease of synthesis, 5,10,15,20-tetrakis-(1-acetamido-4-pyridyl) porphyrin bromide could be considered a betteralternative to TMPyP4 in studies involving G4 binding.
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Citation
CHEMISTRY-A EUROPEAN JOURNAL. 2024, vol. 30, issue 69, p. 1-13.
https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/chem.202402600
https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/chem.202402600
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Peer-reviewed
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Published version
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en
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Defence
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Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
http://creativecommons.org/licenses/by-nc-nd/4.0/