Evidence map›Paper›PMID 34592820›Full record

ArticleJournal of medicinal chemistry2021

Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist.

Mark D Ericson, Skye R Doering, Courtney M Larson, Katie T Freeman, Travis M LaVoi, Haley M Donow, Radleigh G Santos, Rachel H Cho, Zoe M Koerperich, Marc A Giulianotti and 3 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
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  5. 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

13 authors.

Mark D EricsonDepartment of Medicinal Chemistry and Institute for Translation Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.ORCID 0000-0002-8715-6010
Skye R DoeringDepartment of Medicinal Chemistry and Institute for Translation Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.
Courtney M LarsonDepartment of Medicinal Chemistry and Institute for Translation Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.
Katie T FreemanDepartment of Medicinal Chemistry and Institute for Translation Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.
Travis M LaVoiFlorida International University, Port St. Lucie, Florida 34987, United States.
Haley M DonowFlorida International University, Port St. Lucie, Florida 34987, United States.
Radleigh G SantosNova Southeastern University, 3301 College Avenue, Fort Lauderdale, Florida 33314, United States.
Rachel H ChoDepartment of Medicinal Chemistry and Institute for Translation Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.
Zoe M KoerperichDepartment of Medicinal Chemistry and Institute for Translation Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.ORCID 0000-0001-9971-6284
Marc A GiulianottiFlorida International University, Port St. Lucie, Florida 34987, United States.ORCID 0000-0002-2232-3789
Clemencia PinillaFlorida International University, Port St. Lucie, Florida 34987, United States.
Richard A HoughtenFlorida International University, Port St. Lucie, Florida 34987, United States.
Carrie Haskell-LuevanoDepartment of Medicinal Chemistry and Institute for Translation Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.ORCID 0000-0002-6783-5972

Funding

Melanocortin Receptor Selective LigandsR01DK124504 · NIDDK · UNIVERSITY OF MINNESOTA · PI GIULIANOTTI, MARC, HASKELL-LUEVANO, CARRIE · 2021 to 2024
$2.8M
Melanocortin Selective LigandsR01DK091906 · NIDDK · UNIVERSITY OF MINNESOTA · PI HASKELL-LUEVANO, CARRIE · 2012 to 2015
$1.8M
NIDDK NIH HHS R01 DK091906NIDDK NIH HHS R01 DK124504
6 · The paper itself

Abstract

The melanocortin-4 receptor (MC4R) plays an important role in appetite. Agonist ligands that stimulate the MC4R decrease appetite, while antagonist compounds increase food consumption. Herein, a functional mixture-based positional scan identified novel MC4R antagonist sequences. Mixtures comprising a library of 12,960,000 tetrapeptides were screened in the presence and absence of the NDP-MSH agonist. These results led to the synthesis of 48 individual tetrapeptides, of which 40 were screened for functional activity at the melanocortin receptors. Thirteen compounds were found to possess nanomolar antagonist potency at the MC4R, with the general tetrapeptide sequence Ac-Aromatic-Basic-Aromatic-Basic-NH

Indexed as

Agouti-Related ProteinAnimalsComplex MixturesHigh-Throughput Screening AssaysHumansMiceOligopeptidesPeptide FragmentsReceptor, Melanocortin, Type 4Receptors, MelanocortinStructure-Activity RelationshipAgouti-Related Proteinagouti-related protein (86-132), humanComplex MixturesMC4R protein, humanOligopeptidesPeptide FragmentsReceptor, Melanocortin, Type 4Receptors, Melanocortin

Identifiers

PMID34592820
PMCPMC8533642

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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.