Convergent Synthesis of Template-Assembled Synthetic G-Quartets (TASQs) Used as Biomimetic and Multivalent G-Quadruplex (G4) Ligands

模板组装合成G-四联体(TASQs)的汇聚合成及其作为仿生和多价G-四链体(G4)配体的应用

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Abstract

Precise insights into the biology of DNA and RNA G-quadruplexes (G4s) were obtained thanks to the use of ever more versatile G4-interacting molecules (or G4 ligands), which bear additional moieties making them functionalizable in situ (i.e., while in interaction with cellular G4s) thanks to bioorthogonal chemistry. We recently reported on a series of biomimetic G4 ligands known as TASQs (for template-assembled synthetic G-quartets) whose multifunctionality was exploited to visualize (pre-targeted and in situ click imaging) and identify cellular G4s (G4omics and Chem-CLIP). We report herein on a novel synthetic strategy that makes multivalent TASQs readily accessible and opens brand new perspectives for the design of ever smarter molecular tools to unravel the quite complex G4 biology in a more accurate, straightforward, and simpler manner.

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