Development of a Global Reporter on Transcript Abundance (GRETA) for drug discovery and development

Arpeggio Biosciences has developed an automated RNA sequencing platform capable of measuring genome-wide transcript levels for less than $2 per sample. The platform is ideal for measuring the transcriptomic responses to thousands of individual compounds, allowing rapid definition of each compound's mechanism of action. We have successfully used the platform as part of compound screening cascades as well as part of a hit-to-lead campaign resulting in a first-in-class orally bioavailable GPX4 inhibitor for the treatment of drug-resistant cancers. Importantly, GRETA not only quantifies the on-target effects of a compound, but also the diverse off-target effects of a compound - from a single experiment - allowing rapid prioritization of compounds for further exploration.