Introduction to the themed collection on ‘Targeting RNA with small molecules’
Guest Editors Ruth Brenk, Peng Wu and Maria Duca introduce the RSC Medicinal Chemistry themed collection on ‘Targeting RNA with small molecules’.
Inhibition of bacterial RNA polymerase function and protein–protein interactions: a promising approach for next-generation antibacterial therapeutics
The increasing prevalence of multidrug-resistant pathogens necessitates the urgent development of new antimicrobial agents with innovative modes of action for the next generation of antimicrobial therapy.
Small molecules modulating RNA splicing: a review of targets and future perspectives
The review focuses on small molecules that modulate RNA splicing by interacting with a variety of targets, and in the context of disease treatment.
Medicinal chemistry approaches to target the MNK–eIF4E axis in cancer
Cap-dependent translation can become defective and lead to aberrant oncogenic translation and uncontrolled proliferation. We discuss the functions of MNK and eIF4E and recent medicinal chemistry to develop small molecules to target this axis.
Review Article
Oxazolidinones as versatile scaffolds in medicinal chemistry
Oxazolidinone is a five-member heterocyclic ring with several biological applications in medicinal chemistry.
Research Article
A novel aurone RNA CAG binder inhibits the huntingtin RNA–protein interaction
A novel aurone binder for CAG RNA repeats has been identified from a library of twenty-eight compounds. The ligand inhibits toxic RNA–protein interactions in the Huntington's disease model.
Research Article
Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7–Lin28 RNA–protein interaction
Dysregulation of the networking of RNA-binding proteins (RBPs) and RNAs drives many human diseases, including cancers, and the targeting of RNA–protein interactions (RPIs) has emerged as an exciting area of RNA-targeted drug discovery.
Research Article
Structure-based virtual screening of unbiased and RNA-focused libraries to identify new ligands for the HCV IRES model system
Using structure-based virtual screening, FRET and MST assays, novel ligands of the hepatitis C virus internal ribosome entry site were identified. This proof-of-concept study demonstrated the feasibility of RNA–ligand docking for hit identification.
Research Article
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2
SAH-derived bisubstrates of SARS-CoV-2 cap RNA N7-methyltransferase were synthesized, and two adenosines with an N-arylsulfonamide core attached by an N-ethylthioether linker proved to be effective inhibitors in the submicromolar range.
Research Article
Small molecule WDR5 inhibitors down-regulate lncRNA expression
WDR5 inhibitors selective for either one of its binding sites shed light on its role in regulation of lncRNA expression.
Research Article
NMR 1H,19F-based screening of the four stem-looped structure 5_SL1–SL4 located in the 5′-untranslated region of SARS-CoV 2 RNA
Exploring the benefits and limits of ligand based combined 1H and 19F NMR readout for interaction studies of viral RNAs with small compounds.
Development of 2-deoxystreptamine–nucleobase conjugates for the inhibition of oncogenic miRNA production
2-deoxystreptamine (2-DOS) conjugates with artificial nucleobases were designed and synthesized to inhibit pre-miR-372 processing into oncogenic miRNA and were discovered to be promising inhibitors when compared to their neomycin counterpart.
About this collection
This themed collection, guest edited by Dr Maria Duca (Université Côte d’Azur - CNRS, France), Dr Peng Wu (Max Planck Institute of Molecular Physiology, Germany), and Professor Ruth Brenk (University of Bergen, Norway), highlights the latest medicinal chemistry advances in targeting RNA. This collection covers various areas related to the potential of chemical probes and bioactive molecules acting on RNA and RNA-binding proteins, and aims at identifying emerging trends and technologies in the discovery of strong and selective ligands that will advance the RNA targeting field in the next decade.
New articles will be added to the collection upon publication. Please return to this page frequently to see the collection grow.