Optimization of a Protein-Targeted Medicine into an RNA-Specific Small Molecule

• DOI: 10.1021/acschembio.3c00476
• Publication Date: 2023-10-23T17:10:45Z
• Authors: Samantha M. Meyer; Toru Tanaka; Amirhossein Taghavi; Jared T. Baisden; Maison Grefe; Matthew D. Disney
• Keywords: MicroRNAs; Receptor Protein-Tyrosine Kinases; Protein Kinase Inhibitors; 3. Good health

Protein-targeted small molecule medicines often bind RNAs and affect RNA-mediated pathways in cells. Historically, engagement modulation of RNA have not been considered medicine development; however, should be both a potential on- off-target. Kinase inhibitors emecrged as common binders with dovitinib, classic receptor tyrosine kinase (RTK) inhibitor, inhibiting RTKs the biogenesis oncogenic microRNA-21 through direct engagement. In this study, we use knowledge molecular recognition protein targets by dovitinib to design molecules that specifically inhibit target but lack activity against canonical As it is now becoming apparent can an off-target for medicines, study lays foundation principles maximize desired compound while minimizing effects.