DNA G-quadruplexes in the genome of Trypanosoma cruzi as potential therapeutic targets for Chagas disease: Dithienylethene ligands as effective antiparasitic agents

Pérez-Soto, Manuel; Ramos-Soriano, Javier; Peñalver, Pablo; Belmonte-Reche, Efres; O'Hagan, Michael P.; Cucchiarini, Anne; Mergny, Jean-Louis; Galán, M. Carmen; López López, Manuel Carlos; Thomas, María del Carmen; Morales, Juan Carlos

doi:10.1016/j.ejmech.2024.116641

European Journal of Medicinal Chemistry

2024

DOI: 10.1016/j.ejmech.2024.116641

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DNA G-quadruplexes in the genome of Trypanosoma cruzi as potential therapeutic targets for Chagas disease: Dithienylethene ligands as effective antiparasitic agents

Manuel Pérez-Soto,

Javier Ramos-Soriano,

Pablo Peñalver

et al.

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2024

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Cited by 2 publications

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Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design

Ramos-Soriano,

Holbrow-Wilshaw,

Hunt

et al. 2024

Chem. Commun.

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Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design

Ramos-Soriano,

Holbrow-Wilshaw,

Hunt

et al. 2024

Chem. Commun.

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Oligostyrylbenzene Derivatives with Antiparasitic and Antibacterial Activity as Potent G-Quadruplex Ligands

Pérez-Soto,

Peñalver,

Muñoz-Báez

et al. 2024

Molecules

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G-quadruplexes (G4s) are non-canonical secondary structures that play a crucial role in the regulation of genetic expression. This study explores the interaction between G4s and a small family of oligostyrylbenzene (OSB) derivatives, characterized by tris(styryl)benzene and tetrastyrylbenzene backbones, functionalized with either trimethylammonium or 1-methylpyridinium groups. Initially identified as DNA ligands, these OSB derivatives have now been recognized as potent G4 binders, surpassing in binding affinity commercially available ligands such as pyridostatin and displaying good selectivity for G4s over duplex DNA. Furthermore, OSB derivatives 1 and 2 demonstrated significant antiparasitic activity against bloodstream forms of T. brucei and extracellular L. major, with high selectivity indices when compared to MRC-5 healthy control cells. Derivatives 1 and 2 exhibited moderate biocidal effects against a range of Gram-positive and Gram-negative bacterial strains. Notably, a synergistic antibacterial effect was observed when these compounds were combined with traditional antibiotics, particularly against Acinetobacter baumannii, highlighting their potential utility in addressing drug-resistant bacterial infections. The differences in bioactivity among the OSB derivatives can be attributed to variations in cellular uptake, as proved by flow cytometry analysis. This suggests that the degree of cellular internalization plays a pivotal role in the observed antiparasitic and antibacterial efficacy.

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DNA G-quadruplexes in the genome of Trypanosoma cruzi as potential therapeutic targets for Chagas disease: Dithienylethene ligands as effective antiparasitic agents

Cited by 2 publications

References 65 publications

Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design

Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design

Oligostyrylbenzene Derivatives with Antiparasitic and Antibacterial Activity as Potent G-Quadruplex Ligands

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