期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 19, 页码 6786-6795出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm2006904
关键词
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资金
- NIH [GM073188]
- Ohio University
- DAAD
The enantiomers and the cis isomers of two previously studied 4,5-disubstituted oxazolidinones have been synthesized, and their binding to the T-box riboswitch antiterminator model RNA has been investigated in detail. Characterization of ligand affinities and binding site localization indicates that there is little stereospecific discrimination for binding antiterminator RNA alone. This binding similarity between enantiomers is likely due to surface binding, which accommodates ligand conformations 1 that result in comparable ligand-antiterminator contacts. These results have significant implications for T-box antiterminator-targeted drug discovery and, in general, for targeting other medicinally relevant RNA that do not present deep binding pockets.
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