↓ Skip to main content

Dove Medical Press

Article Metrics

Functional characterization of a competitive peptide antagonist of p65 in human macrophage-like cells suggests therapeutic potential for chronic inflammation

Overview of attention for article published in Drug Design, Development and Therapy, December 2014
Altmetric Badge

About this Attention Score

  • Good Attention Score compared to outputs of the same age (74th percentile)
  • Good Attention Score compared to outputs of the same age and source (73rd percentile)

Mentioned by

twitter
2 tweeters
patent
1 patent

Citations

dimensions_citation
8 Dimensions

Readers on

mendeley
22 Mendeley
Title
Functional characterization of a competitive peptide antagonist of p65 in human macrophage-like cells suggests therapeutic potential for chronic inflammation
Published in
Drug Design, Development and Therapy, December 2014
DOI 10.2147/dddt.s59722
Pubmed ID
Authors

Mythily Srinivasan, Debomoy Lahiri, Corrine Blackburn

Abstract

Glucocorticoid-induced leucine zipper (GILZ) is a glucocorticoid responsive protein that links the nuclear factor-kappa B (NFκB) and the glucocorticoid signaling pathways. Functional and binding studies suggest that the proline-rich region at the carboxy terminus of GILZ binds the p65 subunit of NFκB and suppresses the immunoinflammatory response. A widely-used strategy in the discovery of peptide drugs involves exploitation of the complementary surfaces of naturally occurring binding partners. Previously, we observed that a synthetic peptide (GILZ-P) derived from the proline-rich region of GILZ bound activated p65 and ameliorated experimental encephalomyelitis. Here we characterize the secondary structure of GILZ-P by circular dichroic analysis. GILZ-P adopts an extended polyproline type II helical conformation consistent with the structural conformation commonly observed in interfaces of transient intermolecular interactions. To determine the potential application of GILZ-P in humans, we evaluated the toxicity and efficacy of the peptide drug in mature human macrophage-like THP-1 cells. Treatment with GILZ-P at a wide range of concentrations commonly used for peptide drugs was nontoxic as determined by cell viability and apoptosis assays. Functionally, GILZ-P suppressed proliferation and glutamate secretion by activated macrophages by inhibiting nuclear translocation of p65. Collectively, our data suggest that the GILZ-P has therapeutic potential in chronic CNS diseases where persistent inflammation leads to neurodegeneration such as multiple sclerosis and Alzheimer's disease.

Twitter Demographics

The data shown below were collected from the profiles of 2 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 22 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 22 100%

Demographic breakdown

Readers by professional status Count As %
Student > Master 4 18%
Student > Ph. D. Student 3 14%
Librarian 2 9%
Student > Bachelor 2 9%
Lecturer 2 9%
Other 5 23%
Unknown 4 18%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 4 18%
Biochemistry, Genetics and Molecular Biology 4 18%
Agricultural and Biological Sciences 4 18%
Psychology 2 9%
Medicine and Dentistry 1 5%
Other 1 5%
Unknown 6 27%

Attention Score in Context

This research output has an Altmetric Attention Score of 5. 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 15 December 2020.
All research outputs
#4,969,027
of 17,944,974 outputs
Outputs from Drug Design, Development and Therapy
#276
of 1,775 outputs
Outputs of similar age
#92,164
of 362,056 outputs
Outputs of similar age from Drug Design, Development and Therapy
#13
of 46 outputs
Altmetric has tracked 17,944,974 research outputs across all sources so far. This one has received more attention than most of these and is in the 72nd percentile.
So far Altmetric has tracked 1,775 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 5.1. This one has done well, scoring higher than 83% of its peers.
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 362,056 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 74% of its contemporaries.
We're also able to compare this research output to 46 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 73% of its contemporaries.