Abstract

The functional roles of structured RNAs in the regulation of biological processes, and hence RNA's potential as an effective therapeutic target, have only recently been appreciated. Robust and high-throughput methods that identify potent RNA ligands are critical to the development of chemical probes and therapeutics. DNA-encoded libraries (DEL) technology has emerged as a powerful tool for protein ligand discovery, and its ability to generate large, custom-tailored, and novel chemical space offers unprecedented opportunities to discover the rules of RNA ligand design. In this review, we discuss the basic principles of DEL selection, current progress on the application of DEL to RNA targets, and the outlook of targeting RNA by DEL.