ArticleOrganic & biomolecular chemistry2013
Targeting folded RNA: a branched peptide boronic acid that binds to a large surface area of HIV-1 RRE RNA.
Article in Organic & biomolecular chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
12 citing papers in PubMed.
- Peptide Boronic Acids by Late-Stage Hydroboration on the Solid Phase.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Merging the Versatile Functionalities of Boronic Acid with Peptides.International journal of molecular sciences · 2021Review
- Molecular recognition of a branched peptide with HIV-1 Rev Response Element (RRE) RNA.Bioorganic & medicinal chemistry · 2019Article
- Molecular recognition of HIV-1 RNAs with branched peptides.Methods in enzymology · 2019Article
- Discovery of a Branched Peptide That Recognizes the Rev Response Element (RRE) RNA and Blocks HIV-1 Replication.Journal of medicinal chemistry · 2018Article
- Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA.Bioorganic & medicinal chemistry · 2016Article
- Effect of intercalator and Lewis acid-base branched peptide complex formation: boosting affinity towards HIV-1 RRE RNA.MedChemComm · 2016Article
- A structurally plastic ribonucleoprotein complex mediates post-transcriptional gene regulation in HIV-1.Wiley interdisciplinary reviews. RNA · 2016Review
- Review
- HIV-1 drug discovery: targeting folded RNA structures with branched peptides.Organic & biomolecular chemistry · 2015Article
- Targeting the HIV RNA genome: high-hanging fruit only needs a longer ladder.Current topics in microbiology and immunology · 2015Review
- Putting an 'End' to HIV mRNAs: capping and polyadenylation as potential therapeutic targets.AIDS research and therapy · 2013Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
On-bead high-throughput screening of a medium-sized (1000-2000 Da) branched peptide boronic acid (BPBA) library consisting of 46,656 unique sequences against HIV-1 RRE RNA generated peptides with binding affinities in the low micromolar range. In particular, BPBA1 had a K(d) of 1.4 μM with RRE IIB, preference for RNA over DNA (27 fold), and selectivity of up to >75 fold against a panel of RRE IIB variants. Structure-activity studies suggest that the boronic acid moiety and "branching" in peptides are key structural features for efficient binding and selectivity for the folded RNA target. BPBA1 was efficiently taken up by HeLa and A2780 cells. RNA-footprinting studies revealed that the BPBA1 binding site encompasses a large surface area that spans both the upper stem as well as the internal loop regions of RRE IIB.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.