Evidence map›Paper›PMID 26703794›Full record

ArticleEuropean journal of medicinal chemistry2016

Identification of novel cyclic lipopeptides from a positional scanning combinatorial library with enhanced antibacterial and antibiofilm activities.

Nina Bionda, Renee M Fleeman, César de la Fuente-Núñez, Maria C Rodriguez, Fany Reffuveille, Lindsey N Shaw, Irena Pastar, Stephen C Davis, Robert E W Hancock, Predrag Cudic

Abstract read
In one paragraph

Article in European journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.

0numbers the graph read from it
0cells of the map it votes in
27citing papers in PubMed
–field-weighted citation impact
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

27 citing papers in PubMed.

  1. Review
  2. Mapping the knowledge landscape ofFrontiers in cellular and infection microbiology · 2026
    Review
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  5. Article
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  17. Article
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  19. Recent Advances in the Synthesis of Peptoid Macrocycles.Chemistry (Weinheim an der Bergstrasse, Germany) · 2018
    Review
  20. Review
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

10 authors.

Nina BiondaTorrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie 34987-2352, FLA, USA.
Renee M FleemanDepartment of Cell Biology, Microbiology and Molecular Biology, University of South Florida, 4202 East Fowler Avenue, ISA2015, Tampa 33620-5150, FLA, USA.
César de la Fuente-NúñezDepartment of Microbiology and Immunology, Centre for Microbial Diseases and Immunity Research, 232-2259 Lower Mall Research Station, University of British Columbia, Vancouver V6T 1Z4, BC, Canada.
Maria C RodriguezTorrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie 34987-2352, FLA, USA.
Fany ReffuveilleDepartment of Microbiology and Immunology, Centre for Microbial Diseases and Immunity Research, 232-2259 Lower Mall Research Station, University of British Columbia, Vancouver V6T 1Z4, BC, Canada.
Lindsey N ShawDepartment of Cell Biology, Microbiology and Molecular Biology, University of South Florida, 4202 East Fowler Avenue, ISA2015, Tampa 33620-5150, FLA, USA.
Irena PastarDepartment of Dermatology and Cutaneous Surgery, University of Miami Miller School of Medicine, Miami, FLA, USA.
Stephen C DavisDepartment of Dermatology and Cutaneous Surgery, University of Miami Miller School of Medicine, Miami, FLA, USA.
Robert E W HancockDepartment of Microbiology and Immunology, Centre for Microbial Diseases and Immunity Research, 232-2259 Lower Mall Research Station, University of British Columbia, Vancouver V6T 1Z4, BC, Canada.
Predrag CudicTorrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie 34987-2352, FLA, USA. Electronic address: pcudic@tpims.org.

Funding

Novel cyclic lipopeptides for treating gram negative bacterial infectionsR21AI119288 · NIAID · TORREY PINES INST FOR MOLECULAR STUDIES · PI HOUGHTEN, RICHARD ALLEN · 2015 to 2016
$475k
Bioprospecting antibiotics in the fungal secondary metabolomeR21AI103715 · NIAID · UNIVERSITY OF SOUTH FLORIDA · PI BAKER, BILL J, SHAW, LINDSEY NEIL · 2013 to 2014
$391k
NIAID NIH HHS 1R21AI119288-01NIAID NIH HHS AI103715NIAID NIH HHS R21 AI103715NIAID NIH HHS R21 AI119288
6 · The paper itself

Abstract

Treating bacterial infections can be difficult due to innate or acquired resistance mechanisms, and the formation of biofilms. Cyclic lipopeptides derived from fusaricidin/LI-F natural products represent particularly attractive candidates for the development of new antibacterial and antibiofilm agents, with the potential to meet the challenge of bacterial resistance to antibiotics. A positional-scanning combinatorial approach was used to identify the amino acid residues responsible for driving antibacterial activity, and increase the potency of these cyclic lipopeptides. Screening against the antibiotic resistant ESKAPE pathogens revealed the importance of hydrophobic as well as positively charged amino acid residues for activity of this class of peptides. The improvement in potency was especially evident against bacterial biofilms, since the lead cyclic lipopeptide showed promising in vitro and in vivo anti-biofilm activity at the concentration far below its respective MICs. Importantly, structural changes resulting in a more hydrophobic and positively charged analog did not lead to an increase in toxicity toward human cells.

Indexed as

Combinatorial Chemistry TechniquesPeptide LibraryAcinetobacter baumanniiAnti-Bacterial AgentsBiofilmsCell LineCell SurvivalDose-Response Relationship, DrugHumansLipopeptidesMicrobial Sensitivity TestsMolecular StructurePeptides, CyclicPseudomonas aeruginosaStaphylococcus aureusStructure-Activity RelationshipAnti-Bacterial AgentsLipopeptidesPeptide LibraryPeptides, CyclicBiofilmCombinatorial libraryCyclic lipopeptidesPorcine modelResistanceToxicity

Identifiers

PMID26703794
PMCPMC4724249

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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.