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Amphiphilic guanidinocalixarenes inhibit lipopolysaccharide (LPS)- and lectin-stimulated Toll-like Receptor 4 (TLR4) signaling

Overview of attention for article published in Journal of Medicinal Chemistry, May 2017
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Title
Amphiphilic guanidinocalixarenes inhibit lipopolysaccharide (LPS)- and lectin-stimulated Toll-like Receptor 4 (TLR4) signaling
Published in
Journal of Medicinal Chemistry, May 2017
DOI 10.1021/acs.jmedchem.7b00095
Pubmed ID
Authors

Stefania Enza Sestito, Fabio A. Facchini, Ilaria Morbioli, Jean-Marc Billod, Sonsoles Martin Santamaria, Alessandro Casnati, Francesco Sansone, Francesco Peri, Stefania E. Sestito, Sonsoles Martin-Santamaria

Abstract

We recently reported on the activity of cationic amphiphiles in inhibiting TLR4 activation and subsequent production of inflammatory cytokines in cells and in animal models. Starting from the assumption that opportunely designed cationic amphiphiles can behave as CD14/MD-2 ligands and therefore modulate the TLR4 signaling, we present here a panel of amphiphilic guanidinocalixarenes whose structure was computationally optimized to dock into MD-2 and CD14 binding sites. Some of these calixarenes were active in inhibiting, in a dose-dependent way, the LPS-stimulated TLR4 activation and TLR4-dependent cytokine production in human and mouse cells. Moreover, guanidinocalixarenes also inhibited TLR4 signaling when TLR4 was activated by a non-LPS stimulus, the plant lectin PHA. While the activity of guanidinocalixarenes in inhibiting LPS toxic action has previously been related to their capacity to bind LPS, we suggest a direct antagonist effect of calixarenes on TLR4/MD-2 dimerization, pointing at the calixarene moiety as a potential scaffold for the development of new TLR4-directed therapeutics.

Twitter Demographics

The data shown below were collected from the profiles of 3 tweeters who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 2 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 2 100%

Demographic breakdown

Readers by professional status Count As %
Student > Bachelor 1 50%
Professor > Associate Professor 1 50%
Readers by discipline Count As %
Chemistry 2 100%

Attention Score in Context

This research output has an Altmetric Attention Score of 2. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 27 June 2017.
All research outputs
#4,004,851
of 8,430,317 outputs
Outputs from Journal of Medicinal Chemistry
#2,542
of 4,082 outputs
Outputs of similar age
#116,236
of 248,842 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#46
of 85 outputs
Altmetric has tracked 8,430,317 research outputs across all sources so far. This one has received more attention than most of these and is in the 50th percentile.
So far Altmetric has tracked 4,082 research outputs from this source. They receive a mean Attention Score of 4.4. This one is in the 35th percentile – i.e., 35% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 248,842 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 50% of its contemporaries.
We're also able to compare this research output to 85 others from the same source and published within six weeks on either side of this one. This one is in the 42nd percentile – i.e., 42% of its contemporaries scored the same or lower than it.