Evidence map›Paper›PMID 29660981›Full record

ArticleJournal of medicinal chemistry2018

Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.

Francesco Merlino, Yang Zhou, Minying Cai, Alfonso Carotenuto, Ali M Yousif, Diego Brancaccio, Salvatore Di Maro, Silvia Zappavigna, Antonio Limatola, Ettore Novellino and 2 more

Abstract 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 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
–field-weighted citation impact
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

9 citing papers in PubMed.

  1. Article
  2. Carbocyclic setmelanotide analogs maintain biochemical potency at melanocortin 4 receptors.Journal of peptide science : an official publication of the European Peptide Society · 2025
    Article
  3. Article
  4. Article
  5. Demonstration of a Common DPheJournal of medicinal chemistry · 2022
    Article
  6. Article
  7. Article
  8. Article
  9. 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

12 authors.

Francesco MerlinoDepartment of Pharmacy , University of Naples "Federico II" , Via D. Montesano 49 , 80131 Naples , Italy.ORCID 0000-0002-9607-229X
Yang ZhouDepartment of Chemistry and Biochemistry , University of Arizona , 1306 E. University Boulevard , Tucson , Arizona 85721 , United States.
Minying CaiDepartment of Chemistry and Biochemistry , University of Arizona , 1306 E. University Boulevard , Tucson , Arizona 85721 , United States.ORCID 0000-0001-9504-2091
Alfonso CarotenutoDepartment of Pharmacy , University of Naples "Federico II" , Via D. Montesano 49 , 80131 Naples , Italy.ORCID 0000-0001-7532-5449
Ali M YousifDepartment of Pharmacy , University of Naples "Federico II" , Via D. Montesano 49 , 80131 Naples , Italy.
Diego BrancaccioDepartment of Pharmacy , University of Naples "Federico II" , Via D. Montesano 49 , 80131 Naples , Italy.
Salvatore Di MaroDiSTABiF , University of Campania "Luigi Vanvitelli" , Via Vivaldi 43 , 81100 Caserta , Italy.ORCID 0000-0002-9286-4433
Silvia ZappavignaDepartment of Precision Medicine , University of Campania "Luigi Vanvitelli" , Via Costantinopoli 16 , 80138 Naples , Italy.
Antonio LimatolaDepartment of Biology , Stanford University , Stanford , California 94305 , United States.
Ettore NovellinoDepartment of Pharmacy , University of Naples "Federico II" , Via D. Montesano 49 , 80131 Naples , Italy.ORCID 0000-0002-2181-2142
Paolo GriecoDepartment of Pharmacy , University of Naples "Federico II" , Via D. Montesano 49 , 80131 Naples , Italy.ORCID 0000-0002-6854-8123
Victor J HrubyDepartment of Chemistry and Biochemistry , University of Arizona , 1306 E. University Boulevard , Tucson , Arizona 85721 , United States.

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

We report the development of macrocyclic melanocortin derivatives of MT-II and SHU-9119, achieved by modifying the cycle dimension and incorporating constrained amino acids in ring-closing. This study culminated in the discovery of novel agonists/antagonists with an unprecedented activity profile by adding pieces to the puzzle of the melanocortin receptor selectivity. Finally, the resulting 19- and 20-membered rings represent a suitable frame for the design of further therapeutic ligands as selective modulators of the melanocortin system.

Indexed as

Drug DesignAlkylationAmino AcidsHEK293 CellsHumansMacrocyclic CompoundsMolecular Docking SimulationPeptidomimeticsProtein ConformationReceptors, MelanocortinStructure-Activity RelationshipAmino AcidsMacrocyclic CompoundsPeptidomimeticsReceptors, Melanocortin

Identifiers

PMID29660981
PMCPMC5999404

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.