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© Biologie structurale et chimie
Structure du domaine en doigt de zinc de la protéine NEMO, déterminée par Résonance magnétique nucléaire (RMN). Cette protéine jouant un rôle dans des maladies (cancer, inflammation), les connaissances acquises sur sa structure offrent de précieuses informations sur sa fonction.
Publication : Organic & biomolecular chemistry

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

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Organic & biomolecular chemistry - 21 Jan 2021

Reznichenko O, Cucchiarini A, Gabelica V, Granzhan A,

Link to Pubmed [PMID] – 33325973

Link to DOI – 10.1039/d0ob01908a

Org Biomol Chem 2021 01; 19(2): 379-386

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.

https://pubmed.ncbi.nlm.nih.gov/33325973