Discovery of RNA-binding fragments using biolayer interferometry
In our newest paper we describe the development of a fragment screening method for RNA targets.
By: Ruth Brenk, Vipul Panchal and Jan Husmann
Published: (Updated: )
Our paper describing fragment screening for RNA targets using biolayer interferometry (BLI) has been published in RSC Med Chem (external link).
In this paper, we demonstrate the effective use of BLI to investigate RNA–small molecule interactions using three different riboswitches, which are potential targets for novel antibiotics. Furthermore, we describe the successful use of BLI to identify fragment binders of these RNA targets. We combined the BLI experiments with ligand-based NMR as an orthogonal validation method and were able to identify seven competitive fragment binders of the flavin mononucleotide (FMN) riboswitch, each featuring scaffolds distinct from the previously known ligands.
This paper has been included in the special collection "Celebrating the 5th Anniversary of RSC Medicinal Chemistry (external link)" to highlight key advances in medicinal chemistry and drug discovery research in the last 5 years, as well as current breakthroughs and future developments within the field.