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SAR study and conformational analysis of a series of novel peptide G protein‐coupled receptor kinase 2 inhibitors

Overview of attention for article published in Biospectroscopy, October 2013
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  • Good Attention Score compared to outputs of the same age (66th percentile)
  • Above-average Attention Score compared to outputs of the same age and source (58th percentile)

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Title
SAR study and conformational analysis of a series of novel peptide G protein‐coupled receptor kinase 2 inhibitors
Published in
Biospectroscopy, October 2013
DOI 10.1002/bip.22295
Pubmed ID
Authors

Isabel Gomez‐Monterrey, Alfonso Carotenuto, Ersilia Cipolletta, Marina Sala, Ermelinda Vernieri, Antonio Limatola, Alessia Bertamino, Simona Musella, Paolo Grieco, Bruno Trimarco, Ettore Novellino, Guido Iaccarino, Pietro Campiglia

Abstract

G protein-coupled receptor kinase 2 (GRK2) plays a central role in the cellular transduction network. In particular, during chronic heart failure GRK2 is upregulated and believed to contribute to disease progression. Thereby, its inhibition offers a potential therapeutic solution to several pathological conditions. In the present study, we performed a SAR study and a NMR conformational analysis of peptides derived from HJ loop of GRK2 and able to selectively inhibit GRK2. From Ala-scan and d-Ala point replacement, we found that Arg residues don't affect the inhibitory properties, while a d-amino acid at position 5 is key to the activity. Conformational analysis identified two β-turns that involve N-terminal residues, followed by a short extended region. These information can help the design of peptides and peptido-mimetics with enhanced GRK2 inhibition properties. © 2013 Wiley Periodicals, Inc. Biopolymers 101: 121-128, 2014.

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X Demographics

The data shown below were collected from the profiles of 5 X users who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 15 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 15 100%

Demographic breakdown

Readers by professional status Count As %
Professor 3 20%
Professor > Associate Professor 3 20%
Student > Ph. D. Student 2 13%
Student > Doctoral Student 1 7%
Researcher 1 7%
Other 1 7%
Unknown 4 27%
Readers by discipline Count As %
Medicine and Dentistry 3 20%
Agricultural and Biological Sciences 2 13%
Biochemistry, Genetics and Molecular Biology 2 13%
Chemistry 2 13%
Computer Science 1 7%
Other 0 0%
Unknown 5 33%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 4. 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 16 June 2013.
All research outputs
#8,427,513
of 25,374,917 outputs
Outputs from Biospectroscopy
#540
of 1,867 outputs
Outputs of similar age
#75,606
of 224,583 outputs
Outputs of similar age from Biospectroscopy
#12
of 29 outputs
Altmetric has tracked 25,374,917 research outputs across all sources so far. This one has received more attention than most of these and is in the 66th percentile.
So far Altmetric has tracked 1,867 research outputs from this source. They receive a mean Attention Score of 3.8. This one has gotten more attention than average, scoring higher than 71% 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 224,583 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 66% of its contemporaries.
We're also able to compare this research output to 29 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 58% of its contemporaries.