It is impossible to overstate the ubiquity of RNA function in human biology. As such, RNA offers a copious menu of therapeutically compelling targets.  Most therapeutic agents that bind directly to RNA are either antibiotics blocking bacterial ribosome function or oligonucleotides with their attendant pharmaceutical limitations.  Small molecules that penetrate membranes, bind to specific mRNAs and pre-mRNAs, and interdict their function represent an attractive target/ligand modality. To this end, Arrakis is identifying druggable, functionally essential RNA sub-structures in mRNA and druglike small molecules that bind to those structures selectively and thereby modulate their function.  This presentation will focus on some of the unique challenges of drugging RNA, offer some solutions to these challenges, and provide some early data on targets of interest.

Drugging RNA structures with drug-like small molecules

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