Velagapudi, Sai Pradeep; Luo, Yiling; Tran, Tuan; Haniff, Hafeez S.; Nakai, Yoshio; Fallahi, Mohammad; Martinez, Gustavo J.; Childs-Disney, Jessica L.; Disney, Matthew D. published the artcile< Defining RNA-Small Molecule Affinity Landscapes Enables Design of a Small Molecule Inhibitor of an Oncogenic Noncoding RNA>, Related Products of 229009-40-9, the main research area is RNA binding small mol inhibitor preparation antitumor screening.
RNA drug targets are pervasive in cells but methods to design small mols. that target them are sparse. Herein, the authors report a general approach to score the affinity and selectivity of RNA motif-small mol. interactions identified via selection. Named High Throughput Structure-Activity Relationships Through Sequencing (HiT-StARTS), HiT-StARTS is statistical in nature and compares input nucleic acid sequences to selected library members that bind a ligand via high throughput sequencing. The approach allowed facile definition of the fitness landscape of hundreds of thousands of RNA motif-small mol. binding partners. These results were mined against folded RNAs in the human transcriptome and identified an avid interaction between a small mol. and the Dicer nuclease-processing site in the oncogenic microRNA (miR)-18a hairpin precursor, which is a member of the miR-17-92 cluster. Application of the small mol., Targapremir-18a, to prostate cancer cells inhibited production of miR-18a from the cluster, derepressed serine/threonine protein kinase 4 protein (STK4), and triggered apoptosis. Profiling the cellular targets of Targapremir-18a via Chem. Cross Linking and Isolation by Pull Down (Chem-CLIP), a covalent small mol.-RNA cellular profiling approach, and other studies showed specific binding of the compound to the miR-18a precursor, revealing broadly applicable factors that govern small mol. drugging of noncoding RNAs.
ACS Central Science published new progress about Antitumor agents. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Related Products of 229009-40-9.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics