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Article Dans Une Revue Journal of Medicinal Chemistry Année : 2023

Synthesis of Bleomycin-Inspired RNA Ligands Targeting the Biogenesis of Oncogenic miRNAs

Chloé Maucort
  • Fonction : Auteur
Maurinne Bonnet
  • Fonction : Auteur
Jean-Claude Ortuno
  • Fonction : Auteur
Gordon Tucker
  • Fonction : Auteur
Emie Quissac
  • Fonction : Auteur
Maïté Verreault
  • Fonction : Auteur
Stéphane Azoulay
  • Fonction : Auteur
Christophe Di Giorgio
Audrey Di Giorgio
  • Fonction : Auteur
Maria Duca

Résumé

Non-coding RNAs (ncRNAs) play pivotal roles in the regulation of gene expression and represent a promising target for the development of new therapeutic approaches. Among these ncRNAs, microRNAs (miRNAs or miRs) are involved in the regulation of gene expression and their dysregulation has been linked to several diseases such as cancers. Indeed, oncogenic miRNAs are overexpressed in cancer cells thus promoting tumorigenesis and maintenance of cancer stem cells that are resistant to chemotherapy and often responsible for therapeutic failure. Here we describe the design and synthesis of new small-molecule RNA binders able to inhibit the biogenesis of oncogenic miRNAs and targeting efficiently cancer stem cells. Through the biochemical study of their interaction with the target and thanks to intracellular assays, we describe the structure-activity relationships for this new series of RNA ligands and we identify compounds bearing a very promising antiproliferative activity against cancer stem cells.
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Dates et versions

hal-04294399 , version 1 (19-11-2023)

Identifiants

Citer

Chloé Maucort, Maurinne Bonnet, Jean-Claude Ortuno, Gordon Tucker, Emie Quissac, et al.. Synthesis of Bleomycin-Inspired RNA Ligands Targeting the Biogenesis of Oncogenic miRNAs. Journal of Medicinal Chemistry, 2023, 66 (15), pp.10639-10657. ⟨10.1021/acs.jmedchem.3c00797⟩. ⟨hal-04294399⟩

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