Towards a druggable epitranscriptome: Compounds that target RNA modifications in cancer


Por: Berdasco, M and Esteller, M

Publicada: 1 jun 2022 Ahead of Print: 1 jul 2021
Resumen:
Epitranscriptomics is an exciting emerging area that studies biochemical modifications of RNA. The field has been opened up by the technical efforts of the last decade to characterize and quantify RNA modifications, and this has led to a map of post-transcriptional RNA marks in normal cell fate and development. However, the scientific interest has been fuelled by the discovery of aberrant epitranscriptomes associated with human diseases, mainly cancer. The challenge is now to see whether epitrancriptomics offers mechanisms that can be effectively targeted by low MW compounds and are thus druggable. In this review, we will describe the principal RNA modifications (with a focus on mRNA), summarize the latest scientific evidence of their dysregulation in cancer and provide an overview of the state-of-the-art drug discovery to target the epitranscriptome. Finally, we will discuss the principal challenges in the field of chemical biology and drug development to increase the potential of targeted-RNA for clinical benefit.

Filiaciones:
:
 Josep Carreras Leukaemia Res Inst, Epigenet Therapies Grp, Expt & Clin Hematol Program PHEC, Barcelona, Catalonia, Spain

 Bellvitge Biomed Res Inst IDIBELL, Canc Epigenet & Biol Program PEBC, Barcelona, Spain

:
 Josep Carreras Leukaemia Res Inst IJC, Canc Epigenet Grp, Canc & Leukemia Epigenet & Biol Program PEBCL, Barcelona, Catalonia, Spain

 Ctr Invest Biomed Red Canc CIBERONC, Madrid, Spain

 Univ Barcelona, Sch Med & Hlth Sci, Physiol Sci Dept, Barcelona, Spain

 Inst Catalana Recerca & Estudis Avancats ICREA, Barcelona, Spain
ISSN: 00071188





British Journal of Pharmacology
Editorial
Wiley-Blackwell, 111 RIVER ST, HOBOKEN 07030-5774, NJ USA, Estados Unidos America
Tipo de documento: Review
Volumen: 179 Número: 12
Páginas: 2868-2889
WOS Id: 000677771700001
ID de PubMed: 34185879
imagen hybrid, Green Submitted, Green Published

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