Small-molecule modulators of protein-RNA interactions

Wan Gi Byun; Donghyun Lim; Seung Bum Park

doi:10.1016/j.cbpa.2022.102149

Small-molecule modulators of protein-RNA interactions

Curr Opin Chem Biol. 2022 Jun:68:102149. doi: 10.1016/j.cbpa.2022.102149. Epub 2022 May 6.

Authors

Wan Gi Byun¹, Donghyun Lim², Seung Bum Park³

Affiliations

¹ CRI Center for Chemical Proteomics, Department of Chemistry, Seoul National University, Seoul, 08826, Korea(South).
² School of Biopharmaceutical and Medical Sciences, Sungshin University, Seoul, 01133, Korea(South).
³ CRI Center for Chemical Proteomics, Department of Chemistry, Seoul National University, Seoul, 08826, Korea(South). Electronic address: sbpark@snu.ac.kr.

PMID: 35533626
DOI: 10.1016/j.cbpa.2022.102149

Abstract

Protein-RNA interactions (PRIs) play crucial roles in diverse cellular pathways, from transcription to liquid-liquid phase separation, and its dysregulation is associated with a wide range of human disorders. Therefore, there is great emphasis on discovering small-molecule modulators that target unexplored PRIs by developing robust PRI assays. In particular, targeting PRIs could offer innovative solutions to expand the druggable genome, as only a small portion of protein-coding genes are currently targeted by drugs. This review describes the therapeutic potential of targeting PRIs using small molecules, biochemical and cell-based experimental tools for observing PRIs, and several PRI modulators. We also highlight emerging technologies and the challenges in developing PRI modulators.

Keywords: Assay platform; High-throughput screening; Protein–RNA interaction; Small-molecule modulators.

Publication types

Review

MeSH terms

Humans
RNA-Binding Proteins*
Small Molecule Libraries* / pharmacology

Substances

RNA-Binding Proteins
Small Molecule Libraries