Ontology type: schema:ScholarlyArticle Open Access: True
2019-12
AUTHORSFlorent Cochet, Fabio A. Facchini, Lenny Zaffaroni, Jean-Marc Billod, Helena Coelho, Aurora Holgado, Harald Braun, Rudi Beyaert, Roman Jerala, Jesus Jimenez-Barbero, Sonsoles Martin-Santamaria, Francesco Peri
ABSTRACTNew 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. More... »
PAGES919
http://scigraph.springernature.com/pub.10.1038/s41598-018-37421-w
DOIhttp://dx.doi.org/10.1038/s41598-018-37421-w
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PUBMEDhttps://www.ncbi.nlm.nih.gov/pubmed/30696900
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]Download the RDF metadata as: json-ld nt turtle xml License info
JSON-LD is a popular format for linked data which is fully compatible with JSON.
curl -H 'Accept: application/ld+json' 'https://scigraph.springernature.com/pub.10.1038/s41598-018-37421-w'
N-Triples is a line-based linked data format ideal for batch operations.
curl -H 'Accept: application/n-triples' 'https://scigraph.springernature.com/pub.10.1038/s41598-018-37421-w'
Turtle is a human-readable linked data format.
curl -H 'Accept: text/turtle' 'https://scigraph.springernature.com/pub.10.1038/s41598-018-37421-w'
RDF/XML is a standard XML format for linked data.
curl -H 'Accept: application/rdf+xml' 'https://scigraph.springernature.com/pub.10.1038/s41598-018-37421-w'
This table displays all metadata directly associated to this object as RDF triples.
339 TRIPLES
21 PREDICATES
90 URIs
21 LITERALS
9 BLANK NODES