ArticleBiochemistry2012
Click dimers to target HIV TAR RNA conformation.
Article in Biochemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed.
- Synergistic action between peptide-neomycin conjugates and polymyxin B against multidrug-resistant gram-negative pathogens.Frontiers in microbiology · 2025Article
- Design of deep-red emissive forced intercalation-induced light-up peptide as an indicator for the HIV-1 TAR RNA-ligand assay: integration of benzo[c,d]indole-quinoline (BIQ) cyanine dye into Tat peptide.Analytical sciences : the international journal of the Japan Society for Analytical Chemistry · 2024Article
- Parallel G-quadruplex recognition by neomycin.Frontiers in chemistry · 2023Article
- The nuclear transcription factor, TAF7, is a cytoplasmic regulator of protein synthesis.Science advances · 2021Article
- Fluorescent indicator displacement assays to identify and characterize small molecule interactions with RNA.Methods (San Diego, Calif.) · 2019Review
- Review
- Fluorescent peptide displacement as a general assay for screening small molecule libraries against RNA.Organic & biomolecular chemistry · 2019Article
- Non-Natural Linker Configuration in 2,6-Dipeptidyl-Anthraquinones Enhances the Inhibition of TAR RNA Binding/Annealing Activities by HIV-1 NC and Tat Proteins.Bioconjugate chemistry · 2018Article
- Comprehensive review of chemical strategies for the preparation of new aminoglycosides and their biological activities.Chemical Society reviews · 2018Review
- An overview of recent advances in duplex DNA recognition by small molecules.Beilstein journal of organic chemistry · 2018Review
- Utilization of chromic polydiacetylene assemblies as a platform to probe specific binding between drug and RNA.RSC advances · 2017Article
- RNA fragments mimicking tRNA analogs interact with cytochrome c.Molecular biology reports · 2016Article
- Multivalency in the recognition and antagonism of a HIV TAR RNA-TAT assembly using an aminoglycoside benzimidazole scaffold.Organic & biomolecular chemistry · 2016Article
- Arginine-linked neomycin B dimers: synthesis, rRNA binding, and resistance enzyme activity.MedChemComm · 2016Article
- Potent inhibition of miR-27a by neomycin-bisbenzimidazole conjugates.Chemical science · 2015Article
- Influence of linker length and composition on enzymatic activity and ribosomal binding of neomycin dimers.Antimicrobial agents and chemotherapy · 2015Article
- Rapid synthesis, RNA binding, and antibacterial screening of a peptidic-aminosugar (PA) library.ACS chemical biology · 2015Article
- A pH Sensitive High-Throughput Assay for miRNA Binding of a Peptide-Aminoglycoside (PA) Library.PloS one · 2015Article
- Synthesis and evaluation of chloramphenicol homodimers: molecular target, antimicrobial activity, and toxicity against human cells.PloS one · 2015Article
- Multivalent Amino Sugars to Recognize Different TAR RNA Conformations.MedChemComm · 2014Article
Corrections and comments
- Erratum issued
Authors and funding
6 authors.
Funding
Abstract
A series of neomycin dimers have been synthesized using "click chemistry" with varying functionality and length in the linker region to target the human immunodeficiency virus type 1 (HIV-1) TAR RNA region of the HIV virus. The TAR (Trans-Activation Responsive) RNA region, a 59 bp stem-loop structure located at the 5'-end of all nascent viral transcripts, interacts with its target, a key regulatory protein, Tat, and necessitates the replication of HIV-1. Neomycin, an aminosugar, has been shown to exhibit multiple binding sites on TAR RNA. This observation prompted us to design and synthesize a library of triazole-linked neomycin dimers using click chemistry. The binding between neomycin dimers and TAR RNA was characterized using spectroscopic techniques, including FID (fluorescent intercalator displacement), a FRET (fluorescence resonance energy transfer) competitive assay, circular dichroism (CD), and UV thermal denaturation. UV thermal denaturation studies demonstrate that binding of neomycin dimers increases the melting temperature (T(m)) of the HIV TAR RNA up to 10 °C. Ethidium bromide displacement (FID) and a FRET competition assay revealed nanomolar binding affinity between neomycin dimers and HIV TAR RNA, while in case of neomycin, only weak binding was detected. More importantly, most of the dimers exhibited lower IC(50) values toward HIV TAR RNA, when compared to the fluorescent Tat peptide, and show increased selectivity over mutant TAR RNA. Cytopathic effects investigated using MT-2 cells indicate a number of the dimers with high affinity toward TAR show promising anti-HIV activity.
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