Selected article for: "RNA element and small molecule"

Author: Morgan, Brittany S; Forte, Jordan E; Hargrove, Amanda E
Title: Insights into the development of chemical probes for RNA
  • Document date: 2018_9_19
  • ID: wupre5uj_9
    Snippet: Many of the monovalent ligands were discovered through traditional screening methods. Approximately one-third of the RNA:ligand interactions were identified by each of the following approaches: focused-screening (FcS), highthroughput screening (HTS), and HTS followed by lead optimization (HTS-LO) [ Figure 2A ]. In this Survey, FcS is defined by the use of biased libraries, which are typically based on prior knowledge of a particular chemotype bin.....
    Document: Many of the monovalent ligands were discovered through traditional screening methods. Approximately one-third of the RNA:ligand interactions were identified by each of the following approaches: focused-screening (FcS), highthroughput screening (HTS), and HTS followed by lead optimization (HTS-LO) [ Figure 2A ]. In this Survey, FcS is defined by the use of biased libraries, which are typically based on prior knowledge of a particular chemotype binding to an RNA element. In contrast to FcS libraries, molecules specifically designed to explore structureactivity relationships were classified as lead optimization (LO). The starting points for several of the FcS libraries and/or other small molecule identification strategies included RNA-binding natural products, chemical similarity searching, and scaffold-based synthesis [ Figure 2B -D]. We caution that the relative success of these various approaches cannot be evaluated since failed attempts are not typically documented in the literature.

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