Abstract
We describe the design and synthesis of new heterodimeric conjugates, which are comprised of a neomycin B (Neo) stem-binding component and a chloramphenicol (Cam) or linezolid (Lnz) loop-binding component. Some of the heterodimeric conjugates display enhanced affinities to RNA targets and that binding occurs in both stem and loop regions of the RNA. In addition, the results of foot-printing and mutation studies suggest that the enhanced binding affinity of the conjugates is RNA sequence-specific.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetamides / chemistry
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Acetamides / metabolism*
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Acetamides / pharmacology
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Aminoglycosides / chemical synthesis
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Aminoglycosides / chemistry
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Aminoglycosides / metabolism*
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Aminoglycosides / pharmacology
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Chloramphenicol / chemistry
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Chloramphenicol / metabolism*
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Chloramphenicol / pharmacology
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Framycetin / chemistry
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Framycetin / metabolism
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Framycetin / pharmacology
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Linezolid
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Nucleic Acid Conformation
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Oxazolidinones / chemistry
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Oxazolidinones / metabolism*
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Oxazolidinones / pharmacology
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RNA / antagonists & inhibitors
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RNA / chemistry
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RNA / metabolism*
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Acetamides
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Aminoglycosides
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Oxazolidinones
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Framycetin
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RNA
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Chloramphenicol
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Linezolid