Evidence map›Paper›PMID 29605997›Full record

ArticleJournal of medicinal chemistry2018

Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.

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 and 11 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
1.6field-weighted citation impact, top 17% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

19 citing papers in PubMed, 34 citations in OpenAlex.

  1. Review
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  11. Demonstration of a Common DPheJournal of medicinal chemistry · 2022
    Article
  12. Article
  13. Review
  14. Review
  15. Targeting Tumors Using Peptides.Molecules (Basel, Switzerland) · 2020
    Review
  16. Gold(I) Cationization Promotes Ring Opening in Lysine-Containing Cyclic Peptides.Journal of the American Society for Mass Spectrometry · 2019
    Article
  17. Article
  18. Review
  19. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

21 authors at 4 institutions in 4 countries.

Thomas DurekInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.ORCID 0000-0003-0686-227X
Philipp M CrommInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.ORCID 0000-0001-5291-3379
Andrew M WhiteInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.ORCID 0000-0002-9481-1079
Christina I SchroederInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.
Quentin KaasInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.ORCID 0000-0001-9988-6152
Joachim WeidmannInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.
Abdullah Ahmad FuaadInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.
Olivier ChenevalInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.
Peta J HarveyInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.
Norelle L DalyInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.ORCID 0000-0002-4697-6602
Yang ZhouDepartment of Chemistry and Biochemistry , University of Arizona , Tucson , Arizona 85721 , United States.
Anita DellsénMechanistic Biology & Profiling, Discovery Sciences, IMED Biotech Unit , AstraZeneca , Gothenburg 43183 Sweden.
Torben ÖsterlundDiscovery Biology, Discovery Sciences, IMED Biotech Unit , AstraZeneca , Gothenburg 43183 Sweden.
Niklas LarssonDiscovery Biology, Discovery Sciences, IMED Biotech Unit , AstraZeneca , Gothenburg 43183 Sweden.
Laurent KnerrMedicinal Chemistry, Cardiovascular and Metabolic Diseases, IMED Biotech Unit , AstraZeneca , Gothenburg 43183 Sweden.ORCID 0000-0002-4810-8526
Udo BauerMedicinal Chemistry, Cardiovascular and Metabolic Diseases, IMED Biotech Unit , AstraZeneca , Gothenburg 43183 Sweden.
Horst KesslerInstitute for Advanced Study and Center of Integrated Protein Science, Department Chemie , Technische Universität München , Lichtenbergstrasse 4 , 85747 Garching , Germany.ORCID 0000-0002-7292-9789
Minying CaiDepartment of Chemistry and Biochemistry , University of Arizona , Tucson , Arizona 85721 , United States.ORCID 0000-0001-9504-2091
Victor J HrubyDepartment of Chemistry and Biochemistry , University of Arizona , Tucson , Arizona 85721 , United States.
Alleyn T PlowrightMedicinal Chemistry, Cardiovascular and Metabolic Diseases, IMED Biotech Unit , AstraZeneca , Gothenburg 43183 Sweden.
David J CraikInstitute for Molecular Bioscience , The University of Queensland , Brisbane , QLD 4072 , Australia.ORCID 0000-0003-0007-6796
The University of Queensland · AUAstraZeneca (Sweden) · SEUniversity of Arizona · USCenter for Integrated Protein Science Munich · DE

Funding

Supplement for "Designing Novel Melanotropins for New Applications for the Melanocortin System"R01GM108040 · NIGMS · UNIVERSITY OF ARIZONA · PI CAI, MINYING, HRUBY, VICTOR J · 2014 to 2017
$1.2M
NIGMS NIH HHS R01 GM108040
6 · The paper itself

Abstract

Ultrastable 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 toward their activity at MC1R and MC3-5R. Double N-methylated compound 18 showed a p K

Indexed as

Drug DesignHEK293 CellsHelianthusHumansMethylationMolecular StructurePeptides, CyclicReceptor, Melanocortin, Type 1Receptor, Melanocortin, Type 3Structure-Activity RelationshipMC1R protein, humanMC3R protein, humanPeptides, CyclicReceptor, Melanocortin, Type 1Receptor, Melanocortin, Type 3SFTI-1 peptide, sunflower

Identifiers

PMID29605997
PMCPMC5999400
OpenAlexW2794506037

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.