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- W2000076692 abstract "Production of the Gag-Pol polyprotein in human immunodeficiency virus (HIV) requires a −1 ribosomal frameshift, which is directed by a highly conserved RNA stem−loop. Building on our discovery of a set of disulfide-containing peptides that bind this RNA, we describe medicinal chemistry efforts designed to begin to understand the structure−activity relationships and RNA sequence−selectivity relationships associated with these compounds. Additionally, we have prepared analogues incorporating an olefin or saturated hydrocarbon bioisostere of the disulfide moiety, as a first step toward enhancing biostability. The olefin-containing compounds exhibit affinity comparable to the lead disulfide and, importantly, have no discernible toxicity when incubated with human fibroblasts at concentrations up to 1 mM." @default.
- W2000076692 created "2016-06-24" @default.
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- W2000076692 date "2010-07-30" @default.
- W2000076692 modified "2023-09-26" @default.
- W2000076692 title "Strategies for Recognition of Stem−Loop RNA Structures by Synthetic Ligands: Application to the HIV-1 Frameshift Stimulatory Sequence" @default.
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- W2000076692 doi "https://doi.org/10.1021/jm100231t" @default.
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