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Towards a druggable epitranscriptome: Compounds that target RNA modifications in cancer
María Berdasco1,2, Manel Esteller3,4,5,6
1Epigenetic Therapies Group, Experimental and Clinical Hematology Program (PHEC), Josep Carreras Leukaemia Research Institute, Barcelona, Spain.
British Journal of Pharmacology
|June 29, 2021
Summary
Epitranscriptomics studies RNA modifications, revealing their role in cancer. This review explores targeting these RNA marks with drugs for cancer treatment, highlighting current challenges and future potential.
Area of Science:
- Biochemistry and Molecular Biology
- Cancer Research
- Pharmacology
Background:
- Epitranscriptomics investigates biochemical modifications of RNA, providing insights into cellular processes.
- Recent advancements enable characterization and quantification of RNA modifications.
- Aberrant epitranscriptomes are increasingly linked to human diseases, particularly cancer.
Purpose of the Study:
- To review key RNA modifications, focusing on mRNA.
- To summarize evidence of RNA modification dysregulation in cancer.
- To provide an overview of drug discovery efforts targeting the epitranscriptome.
Main Methods:
- Literature review of epitranscriptomic research.
- Analysis of scientific evidence linking RNA modifications to cancer.
- Survey of current drug discovery strategies for epitranscriptomic targets.
Main Results:
- Detailed description of principal RNA modifications, especially on mRNA.
- Compilation of data showing RNA modification alterations in various cancers.
- Overview of the current landscape of small molecule compounds targeting the epitranscriptome.
Conclusions:
- Epitranscriptomics presents potential therapeutic targets for cancer.
- Targeting RNA modifications with low molecular weight compounds is a promising, yet challenging, area.
- Further advancements in chemical biology and drug development are crucial for clinical translation.
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