Towards a “druggable” epitranscriptome: Compounds that target RNA
modifications in cancer
Abstract
Epitranscriptomics is an exciting emerging area that studies biochemical
modifications of RNA. The field is boosted by the technical efforts of
the last decade to characterize and quantify RNA modifications which
have led to a map of post-transcripcional RNA marks in normal cell fate
and develoment. However, the scientific interest has been fueled by the
discovery of aberrant epitranscriptomes associated with human diseases,
mainly cancer. The challenge is now to see whether epitrancriptomics
offers a tunable mechanims to be targeted by small- molecule
intervention. In this review, we will describe the principal RNA
modifications (with a focus on mRNA), summarize the latest scientific
evidences 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.