Developing sensitive arrays to facilitate hit identification of RNA modifying enzymes

To facilitate and accelerate drug discovery efforts in this area, we have developed several sensitive and robust assays suitable for identifying and assessing chemical matter against the RNA modifying enzymes FTO and METTL3/METTL14

Schematic representing the role of FTO and METTL3/METTL14 in the regulation of the transcriptome via removal of the m6A modification from RNA.

An MST assay was developed, validated and used to screen 100 compounds from the LOPAC for novel human FTO small molecule binders.

Our proof of concept study describes the development of several robust and sensitive assays for hit identification and
further characterisation of inhibitors of key RNA modifying enzymes and offers a platform for the discovery and
development of novel therapeutics in this emerging area of research.