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The Synergistic Effect of N2 and N7 Modifications on the Inhibitory Efficacy of mRNA Cap Analogues.
Kurpiejewski, Karol; Piecyk, Karolina; Lukaszewicz, Maciej; Kamel, Karol; Chmurski, Kazimierz; Kmiecik, Sebastian; Jankowska-Anyszka, Marzena.
Afiliación
  • Kurpiejewski K; Faculty of Chemistry, University of Warsaw, 02-093 Warsaw, Poland.
  • Piecyk K; Faculty of Chemistry, University of Warsaw, 02-093 Warsaw, Poland.
  • Lukaszewicz M; Division of Biophysics, Institute of Experimental Physics, University of Warsaw, 02-093 Warsaw, Poland.
  • Kamel K; Institute of Bioorganic Chemistry, Polish Academy of Sciences, 61-704 Poznan, Poland.
  • Chmurski K; Faculty of Chemistry, University of Warsaw, 02-093 Warsaw, Poland.
  • Kmiecik S; Biological and Chemical Research Centre, Faculty of Chemistry, University of Warsaw, 02-089 Warsaw, Poland.
  • Jankowska-Anyszka M; Faculty of Chemistry, University of Warsaw, 02-093 Warsaw, Poland.
Pharmaceuticals (Basel) ; 17(5)2024 May 14.
Article en En | MEDLINE | ID: mdl-38794202
ABSTRACT
In the fight against cancer, researchers have turned their attention to the eukaryotic initiation factor eIF4E, a protein whose increased level is strongly correlated with the development and progression of various types of cancer. Among the numerous strategies devised to tackle eIF4E overexpression, the use of 5' end mRNA cap analogues has emerged as a promising approach. Here, we present new candidates as potent m7GMP analogues for inhibiting translation and interfacing with eIF4E. By employing an appropriate strategy, we synthesized doubly modified mono- and dinucleotide cap analogues, introducing simultaneous substituents at both the N7 and N2 positions of the guanine ring. This approach was identified as an effective and promising combination. Our findings reveal that these dual modifications increase the potency of the dinucleotide analogue, marking a significant advancement in the development of cancer therapeutics targeting the eIF4E pathway.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Pharmaceuticals (Basel) Año: 2024 Tipo del documento: Article País de afiliación: Polonia Pais de publicación: Suiza
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Pharmaceuticals (Basel) Año: 2024 Tipo del documento: Article País de afiliación: Polonia Pais de publicación: Suiza