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

Title: Convergent Synthesis of Template‐Assembled Synthetic G‐Quartets (TASQs) Used as Biomimetic and Multivalent G‐Quadruplex (G4) Ligands
Authors: Raevens, Sandy; Desingle, Cécile; Pirrotta, Marc; Sperti, Francesco, Rota; Pieri, Andréa; Lejault, Pauline; Valverde, Ibai, E; Monchaud, David
Contributors: Institut de Chimie Moléculaire de l'Université de Bourgogne Dijon (ICMUB); Institut de Chimie - CNRS Chimie (INC-CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université Bourgogne Europe (UBE); This work was supported by the CNRS MITI (to S.R. and D.M.), CNRS (to I.E.V. and D.M.), UBE (to C.D. and M.P.), Agence Nationale de la Recherche (to D.M., ANR-22-CE44-0039-01 and ANR-24-CE44-1817-03) and Ligue contre le Cancer (to D.M.). The authors thank Prof. Franck Denat for helpful discussions and Baptiste Dupouy for his help in the AMC synthesis.; ANR-24-CE44-1817,TOP2-G4,Comprendre et moduler les propriétés cellulaires des ligands de G-quadruplexes(2024); ANR-22-CE44-0039,InJUNCTION,Des outils moléculaires pour l'étude des jonctions d'ADN(2022)
Source: ISSN: 0947-6539.
Publisher Information: CCSD; Wiley-VCH Verlag
Publication Year: 2025
Collection: Université de Bourgogne (UB): HAL
Subject Terms: macrocycles; chemical biology; molecular tools; synthetic G-quartet; TASQ; Synthesis design; G-quadruplexes; [CHIM]Chemical Sciences
Description: International audience ; 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.
Document Type: article in journal/newspaper
Language: English
Relation: info:eu-repo/semantics/altIdentifier/pmid/41267487; PUBMED: 41267487
DOI: 10.1002/chem.202503002
Availability: https://hal.science/hal-05384162; https://hal.science/hal-05384162v1/document; https://hal.science/hal-05384162v1/file/DM%20-%20CAEJ%20-%202025%20-%20in%20press.pdf; https://doi.org/10.1002/chem.202503002
Rights: http://creativecommons.org/licenses/by/ ; info:eu-repo/semantics/OpenAccess
Accession Number: edsbas.6DBAE012
Database: BASE