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X Demographics
Mendeley readers
Attention Score in Context
| Title |
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor‑1
|
|---|---|
| Published in |
Journal of Medicinal Chemistry, March 2018
|
| DOI | 10.1021/acs.jmedchem.8b00170 |
| Pubmed ID | |
| Authors |
Thomas Durek, Philipp M. Cromm, Andrew M. White, Christina I. Schroeder, Quentin Kaas, Joachim Weidmann, Abdullah Ahmad Fuaad, Olivier Cheneval, Peta J. Harvey, Norelle L. Daly, Yang Zhou, Anita Dellsén, Torben Österlund, Niklas Larsson, Laurent Knerr, Udo Bauer, Horst Kessler, Minying Cai, Victor J. Hruby, Alleyn T. Plowright, David J. Craik |
| Abstract |
Ultra-stable cyclic peptide frameworks offer great potential for drug design due to their improved bioavailability compared to their linear analogues. Using the sunflower trypsin inhibitor-1 (SFTI-1) peptide scaffold in combination with systematic N-methylation of the grafted pharmacophore led to the identification of novel subtype selective melanocortin receptor (MCR) agonists. Multiple bicyclic peptides were synthesized and tested towards their activity at MC1R and MC3-5R. Double N-methylated compound 18 showed a pKi of 8.73±0.08 (Ki = 1.92±0.34 nM) and a pEC50 of 9.13±0.04 (EC50 = 0.75±0.08 nM) at the human MC1R and was over 100 times more selective for MCR1. NMR structural analysis of 18 emphasized the role of peptide bond N-methylation in shaping the conformation of the grafted pharmacophore. More broadly, this study highlights the potential of cyclic peptide scaffolds for epitope grafting in combination with N-methylation to introduce receptor subtype selectivity in the context of peptide-based drug discovery. |
X Demographics
The data shown below were collected from the profiles of 2 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 2 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Scientists | 1 | 50% |
| Members of the public | 1 | 50% |
Mendeley readers
The data shown below were compiled from readership statistics for 37 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 37 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 9 | 24% |
| Student > Ph. D. Student | 9 | 24% |
| Student > Master | 6 | 16% |
| Student > Postgraduate | 2 | 5% |
| Lecturer | 1 | 3% |
| Other | 2 | 5% |
| Unknown | 8 | 22% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 13 | 35% |
| Biochemistry, Genetics and Molecular Biology | 4 | 11% |
| Pharmacology, Toxicology and Pharmaceutical Science | 3 | 8% |
| Medicine and Dentistry | 3 | 8% |
| Agricultural and Biological Sciences | 1 | 3% |
| Other | 3 | 8% |
| Unknown | 10 | 27% |
Attention Score in Context
This research output has an Altmetric Attention Score of 6. 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 01 November 2020.
All research outputs
#5,609,913
of 23,041,514 outputs
Outputs from Journal of Medicinal Chemistry
#11,650
of 22,144 outputs
Outputs of similar age
#97,771
of 329,982 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#57
of 141 outputs
Altmetric has tracked 23,041,514 research outputs across all sources so far. Compared to these this one has done well and is in the 75th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 22,144 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.7. This one is in the 47th percentile – i.e., 47% 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 329,982 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 70% of its contemporaries.
We're also able to compare this research output to 141 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.