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Quadruplex DNA-guided ligand selection from dynamic combinatorial libraries of acylhydrazones

Abstract : Dynamic combinatorial libraries of acylhydrazones were prepared from diacylhydrazides and several cationic or neutral aldehydes in the presence of 5-methoxyanthranilic acid catalyst. Pull-down experiments with magnetic beads functionalized with a G-quadruplex (G4)-forming oligonucleotide led to the identification of putative ligands, which were resynthesized or emulated by close structural analogues. G4-binding properties of novel derivatives were assessed by fluorimetric titrations, mass spectrometry and thermal denaturation experiments, giving evidence of strong binding (Kd < 10 nM) for two compounds.
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https://hal.archives-ouvertes.fr/hal-03186431
Contributor : Anton Granzhan <>
Submitted on : Monday, July 26, 2021 - 3:12:13 PM
Last modification on : Tuesday, July 27, 2021 - 11:33:28 AM

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Oksana Reznichenko, Anne Cucchiarini, Valérie Gabelica, Anton Granzhan. Quadruplex DNA-guided ligand selection from dynamic combinatorial libraries of acylhydrazones. Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2021, 19 (2), pp.379-386. ⟨10.1039/D0OB01908A⟩. ⟨hal-03186431⟩

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