Screening for Small-Molecule Modulators of Long Noncoding RNA-Protein Interactions Using AlphaScreen

In this study, we developed a tool to study lncRNA-protein interactions for high-throughput screening of small-molecule modulators using AlphaScreen technology. We tested the interaction of two lncRNAs: brain-derived neurotrophic factor antisense (BDNF-AS) and Hox transcript antisense RNA (HOTAIR), with Enhancer of zeste homolog 2 (EZH2), a histone methyltransferase against a phytochemical library, to look for small-molecule inhibitors that can alter the expression of downstream target genes. We identified ellipticine, a compound that up-regulates BDNF transcription. Our study shows the feasibility of using high-throughput screening to identify modulators of lncRNA-protein interactions and paves the road for targeting lncRNAs that are dysregulated in human disorders using small-molecule therapies.

http://jbx.sagepub.com/cgi/content/abstract/20/9/1132?rss=1

Source: Journal of Biomolecular Screening - September 18, 2015 Category: Molecular Biology Authors: Pedram Fatemi, R., Salah-Uddin, S., Modarresi, F., Khoury, N., Wahlestedt, C., Faghihi, M. A. Tags: Original Research Source Type: research