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
hybrid, Green Submitted, Green Published
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