RNA-binding fluorogenic probes: G-clamp conjugated with a thiazole orange derivative for screening RNA-binding small molecules.

ABSTRACT: RNA has emerged as an attractive target for drug discovery, increasing the importance of methods for identifying RNA-binding small molecules. Fluorescent indicator displacement (FID) assays are commonly used for screening such molecules. However, because fluorescent indicators detect hit compounds through competitive binding, developing a diverse range of indicators is essential to avoid missing potential hits. Here, we introduce novel RNA-binding fluorogenic molecular probes for FID assays by conjugating thiazole orange (TO) derivatives to the unique RNA-binding molecule G-clamp, resulting in TO-G-clamp. G-clamp was chosen for its distinct RNA-binding mode compared to TO derivatives, as demonstrated by their large-scale RNA-binding profiles. Four TO-G-clamp analogs were synthesized and ev

SUBMITTER: Nagasawa R 

PROVIDER: S-EPMC12580927 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature