ArticleACS chemical biology2015
Rapid synthesis, RNA binding, and antibacterial screening of a peptidic-aminosugar (PA) library.
Article in ACS chemical biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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Who cites it
19 citing papers in PubMed.
- Aminoglycoside-Peptide Nucleic Acid (PNA) Conjugates against Gram-Negative Bacteria.Bioconjugate chemistry · 2025Article
- Synergistic action between peptide-neomycin conjugates and polymyxin B against multidrug-resistant gram-negative pathogens.Frontiers in microbiology · 2025Article
- Conjugates of Aminoglycosides with Stapled Peptides as a Way to Target Antibiotic-Resistant Bacteria.ACS omega · 2023Article
- High-Throughput Screening of Natural Product and Synthetic Molecule Libraries for Antibacterial Drug Discovery.Metabolites · 2023Review
- New 3,4-International journal of molecular sciences · 2023Article
- Spongenolactones A-C, Bioactive 5,5,6,6,5-Pentacyclic Spongian Diterpenes from the Red Sea SpongeMarine drugs · 2022Article
- The Chemically Highly Diversified Metabolites from the Red Sea Marine SpongeMarine drugs · 2022Article
- Fine-tuning miR-21 expression and inhibition of EMT in breast cancer cells using aromatic-neomycin derivatives.Molecular therapy. Nucleic acids · 2022Article
- Potential for the Development of a New Generation of Aminoglycoside Antibiotics.Pharmaceutical chemistry journal · 2021Article
- Template-guided selection of RNA ligands using imine-based dynamic combinatorial chemistry.Chemical communications (Cambridge, England) · 2020Article
- Surface Dependent Dual Recognition of a G-quadruplex DNA With Neomycin-Intercalator Conjugates.Frontiers in chemistry · 2020Article
- Fluorescent indicator displacement assays to identify and characterize small molecule interactions with RNA.Methods (San Diego, Calif.) · 2019Review
- Rapid Solid-phase Syntheses of Peptidic-Aminoglycoside Library.Tetrahedron · 2018Article
- Comprehensive review of chemical strategies for the preparation of new aminoglycosides and their biological activities.Chemical Society reviews · 2018Review
- High Add Valued Application of Turpentine in Crop Production through Structural Modification and QSAR Analysis.Molecules (Basel, Switzerland) · 2018Article
- Antimicrobial Activity, AME Resistance, and A-Site Binding Studies of Anthraquinone-Neomycin Conjugates.ACS infectious diseases · 2017Article
- Arginine-linked neomycin B dimers: synthesis, rRNA binding, and resistance enzyme activity.MedChemComm · 2016Article
- A pH Sensitive High-Throughput Assay for miRNA Binding of a Peptide-Aminoglycoside (PA) Library.PloS one · 2015Article
- A review of patents (2011-2015) towards combating resistance to and toxicity of aminoglycosides.MedChemCommArticle
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
A 215-member mono- and diamino acid peptidic-aminosugar (PA) library, with neomycin as the model aminosugar, was systematically and rapidly synthesized via solid phase synthesis. Antibacterial activities of the PA library, on 13 bacterial strains (seven Gram-positive and six Gram-negative bacterial strains), and binding affinities of the PA library for a 27-base model of the bacterial 16S ribosomal A-site RNA were evaluated using high-throughput screening. The results of the two assays were correlated using Ribosomal Binding-Bacterial Inhibition Plot (RB-BIP) analysis to provide structure-activity relationship (SAR) information. From this work, we have identified PAs that can discriminate the E. coli A-site from the human A-site by up to a 28-fold difference in binding affinity. Aminoglycoside-modifying enzyme activity studies indicate that APH(2″)-Ia showed nearly complete removal of activity with a number of PAs. The synthesis of the compound library and screening can both be performed rapidly, allowing for an iterative process of aminoglycoside synthesis and screening of PA libraries for optimal binding and antibacterial activity for lead identification.
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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.