Inhibitors Library. RNA-Protein Interaction.

ChemDiv’s RNA-Protein Interaction Inhibitor Library contains 2,111 compounds.

RNA binding proteins (RBPs) are a large and diverse class of proteins that regulate all aspects of RNA biology. Since many human conditions, such as malignancies and neurological diseases, have been linked to RBP dysregulation, small molecule chemical probes that specifically target individual RBPs are valuable resources for understanding RNA:protein interactions and directing a promising strategy to develop novel classes of drug candidates.

Targeting RBPs with small-molecule inhibitors is still an emerging and promising research area in comparison to targeting other protein classes, such as G-protein-coupled receptors, ion channels, and kinases. Along with direct regulation of the RNA activity via RBPs engagement, RBPs inhibitors are capable to consequentially affect those types of RNA:protein interactions that cannot be targeted with existing small molecule structures. They also offer an alternative method to target specific RNA:protein interactions that can be targeted with existing modulating ligands. Recent advancements have markedly enhanced understanding of the complex regulatory network of the RNA:protein interactions, alongside clearing the diverse functional mechanisms inherent to various classes of RBPs. This progression has been facilitated by the development and refinement of novel biochemical and cellular assays, which are crucial for the validation of potential molecular interactions and functional roles. As a result, small-molecule modulators targeting numerous RBPs, previously deemed 'unligandable', have been successfully identified and characterized.

Our database contains small-molecule inhibitor compounds targeting several emerging classes of RBPs, including microRNA-binding protein LIN28, dual-stranded RNA-binding or single-stranded RNA-binding Toll-Like Receptors (TLRs), and CRISPR-related RNA (crRNA)-binding Cas proteins. Those inhibitors mark a significant milestone in the field and offer new avenues for therapeutic intervention into RNA-mediated cellular processes.