Evidence map›Paper›PMID 25055981›Full record

ArticleChemMedChem2014

Singly modified amikacin and tobramycin derivatives show increased rRNA A-site binding and higher potency against resistant bacteria.

Richard J Fair, Lisa S McCoy, Mary E Hensler, Bernice Aguilar, Victor Nizet, Yitzhak Tor

Open access · greenAbstract read
In one paragraph

Article in ChemMedChem, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
0.7field-weighted citation impact, top 35% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

10 citing papers in PubMed, 20 citations in OpenAlex.

  1. Article
  2. Article
  3. Complete genome sequence of pathogenicMicrobiology resource announcements · 2025
    Article
  4. Article
  5. Article
  6. Review
  7. Review
  8. Amikacin: Uses, Resistance, and Prospects for Inhibition.Molecules (Basel, Switzerland) · 2017
    Review
  9. Review
  10. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors at 1 institution in 1 country.

Richard J FairDepartment of Chemistry & Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093 (USA).
Lisa S McCoy
Mary E Hensler
Bernice Aguilar
Victor Nizet
Yitzhak Tor
University of California, San Diego · US

Funding

UCSD/SDSU IRACDAK12GM068524 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI TREJO, JOANN · 2003 to 2025
$24.4M
Fluorescent Nucleosides and OligonucleotidesR01GM069773 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI TOR, YITZHAK · 2004 to 2020
$5.0M
TRAINING & OUTREACH COREU54HD071600 · NICHD · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI BEST, BROOKIE MANNING · 2011 to 2015
$3.6M
NICHD NIH HHS HD071600NICHD NIH HHS U54 HD071600NIGMS NIH HHS GM069773NIGMS NIH HHS K12 GM068524NIGMS NIH HHS R01 GM069773
6 · The paper itself

Abstract

Semisynthetic derivatives of the clinically useful aminoglycosides tobramycin and amikacin were prepared by selectively modifying their 6'' positions with a variety of hydrogen bond donors and acceptors. Their binding to the rRNA A-site was probed using an in vitro FRET-based assay, and their antibacterial activities against several resistant strains (e.g., Pseudomonas aeruginosa, Klebsiella pneumonia, MRSA) were quantified by determining minimum inhibitory concentrations (MICs). The most potent derivatives were evaluated for their eukaryotic cytotoxicity. Most analogues displayed higher affinity for the bacterial A-site than the parent compounds. Although most tobramycin analogues exhibited no improvement in antibacterial activity, several amikacin analogues showed potent and broad-spectrum antibacterial activity against resistant bacteria. Derivatives tested for eukaryotic cytotoxicity exhibited minimal toxicity, similar to the parent compounds.

Indexed as

AmikacinAnti-Bacterial AgentsAntibiotics, AntineoplasticBacteriaBinding SitesCell SurvivalDrug Resistance, BacterialModels, MolecularMolecular ConformationRNA, Ribosomal, 16STobramycinAmikacinAnti-Bacterial AgentsAntibiotics, AntineoplasticRNA, Ribosomal, 16STobramycinaminoglycosidesantibioticsA-site rRNAdrug-resistant bacteria

Identifiers

PMID25055981
PMCPMC4298452
OpenAlexW2166277363

What OpenQuestion holds

Textmetadata
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Read underepoch 390

Registered trials

None linked

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.