Discovery of Inhibitors of MicroRNA-21 Processing Using Small Molecule Microarrays.

ABSTRACT: The identification of small molecules that bind to and perturb the function of microRNAs is an attractive approach for the treatment for microRNA-associated pathologies. However, there are only a few small molecules known to interact directly with microRNAs. Here, we report the use of a small molecule microarray (SMM) screening approach to identify low molecular weight compounds that directly bind to a pre-miR-21 hairpin. Compounds identified using this approach exhibit good affinity for the RNA (ranging from 0.8-2.0 μM) and are not composed of a polycationic scaffold. Several of the highest affinity compounds inhibit Dicer-mediated processing, while in-line probing experiments indicate that the compounds bind to the apical loop of the hairpin, proximal to the Dicer site. This work provide

SUBMITTER: Connelly CM 

PROVIDER: S-EPMC6341489 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature