Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 16, Pages 6018-6027Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm100231t
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Funding
- NIH/NIAID via the University of Rochester Developmental Center for AIDS Research (DCFAR) [P30AI078498]
- NIH [T32A R007472]
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [0946653] Funding Source: National Science Foundation
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Production of the Gag-Pol polyprotein in human immunodeficiency virus (HIV) requires a -1 ribosomal frameshift, which is directed by a highly conserved RNA stern-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.
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