Evidence map›Paper›PMID 30696900›Full record

ArticleScientific reports2019

Novel carboxylate-based glycolipids: TLR4 antagonism, MD-2 binding and self-assembly properties.

Florent Cochet, Fabio A Facchini, Lenny Zaffaroni, Jean-Marc Billod, Helena Coelho, Aurora Holgado, Harald Braun, Rudi Beyaert, Roman Jerala, Jesus Jimenez-Barbero and 2 more

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
1.5field-weighted citation impact, top 18% 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

17 citing papers in PubMed, 34 citations in OpenAlex.

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  6. In Vitro Anti-Inflammatory Study of Limonoids Isolated fromCurrent issues in molecular biology · 2024
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  10. Computational and structural biotechnology journal · 2022
    Review
  11. HSP60-Derived Peptide as an LPS/TLR4 Modulator: AnFrontiers in cardiovascular medicine · 2022
    Article
  12. Review
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  15. Review
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  17. 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

12 authors at 6 institutions in 5 countries.

Florent CochetDepartment of Biotechnology and Biosciences, University of Milano-Bicocca, Piazza della Scienza, 2, 20126, Milano, Italy.ORCID 0000-0001-9470-2350
Fabio A FacchiniDepartment of Biotechnology and Biosciences, University of Milano-Bicocca, Piazza della Scienza, 2, 20126, Milano, Italy.
Lenny ZaffaroniDepartment of Biotechnology and Biosciences, University of Milano-Bicocca, Piazza della Scienza, 2, 20126, Milano, Italy.
Jean-Marc BillodDepartment of Structural and Chemical Biology, Centro de Investigaciones Biologicas, CIB-CSIC, Ramiro de Maeztu, 9, 28040, Madrid, Spain.
Helena CoelhoMolecular Recognition & Host-Pathogen Interactions Programme, CIC bioGUNE, Bizkaia Technology Park, Building 801 A, 48170, Derio, Spain.ORCID 0000-0003-1992-8557
Aurora HolgadoUnit for Molecular Signal Transduction in Inflammation VIB-UGent Center for Inflammation Research, VIB Technologiepark 927, 9052, Zwijnaarde, Ghent, Belgium.
Harald BraunUnit for Molecular Signal Transduction in Inflammation VIB-UGent Center for Inflammation Research, VIB Technologiepark 927, 9052, Zwijnaarde, Ghent, Belgium.
Rudi BeyaertUnit for Molecular Signal Transduction in Inflammation VIB-UGent Center for Inflammation Research, VIB Technologiepark 927, 9052, Zwijnaarde, Ghent, Belgium.
Roman JeralaDepartment of Biotechnology, National Institute of Chemistry, Hajdrihova 19, 1000, Ljubljana, Slovenia.ORCID 0000-0002-6337-5251
Jesus Jimenez-BarberoMolecular Recognition & Host-Pathogen Interactions Programme, CIC bioGUNE, Bizkaia Technology Park, Building 801 A, 48170, Derio, Spain.ORCID 0000-0001-5421-8513
Sonsoles Martin-SantamariaDepartment of Structural and Chemical Biology, Centro de Investigaciones Biologicas, CIB-CSIC, Ramiro de Maeztu, 9, 28040, Madrid, Spain.
Francesco PeriDepartment of Biotechnology and Biosciences, University of Milano-Bicocca, Piazza della Scienza, 2, 20126, Milano, Italy. francesco.peri@unimib.it.
University of Milano-Bicocca · ITGhent University · BECentro de Investigaciones Biológicas Margarita Salas · ESIkerbasque · ESNational Institute of Chemistry · SIUniversity of the Basque Country · ES

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

New monosaccharide-based lipid A analogues were rationally designed through MD-2 docking studies. A panel of compounds with two carboxylate groups as phosphates bioisosteres, was synthesized with the same glucosamine-bis-succinyl core linked to different unsaturated and saturated fatty acid chains. The binding of the synthetic compounds to purified, functional recombinant human MD-2 was studied by four independent methods. All compounds bound to MD-2 with similar affinities and inhibited in a concentration-dependent manner the LPS-stimulated TLR4 signaling in human and murine cells, while being inactive as TLR4 agonists when provided alone. A compound of the panel was tested in vivo and was not able to inhibit the production of proinflammatory cytokines in animals. This lack of activity is probably due to strong binding to serum albumin, as suggested by cell experiments in the presence of the serum. The interesting self-assembly property in solution of this type of compounds was investigated by computational methods and microscopy, and formation of large vesicles was observed by cryo-TEM microscopy.

Indexed as

AnimalsBinding SitesGlycolipidsHumansLymphocyte Antigen 96MacrophagesMiceMolecular ConformationMolecular Docking SimulationMolecular Dynamics SimulationMolecular StructureProtein BindingSignal TransductionStructure-Activity RelationshipToll-Like Receptor 4GlycolipidsLymphocyte Antigen 96Toll-Like Receptor 4

Identifiers

PMID30696900
PMCPMC6351529
OpenAlexW2913968866

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.