Evidence map›Paper›PMID 39795070›Full record

ArticleMolecules (Basel, Switzerland)2024

Design, Structure-Activity Relationships, and Computational Modeling Studies of a Series of α-Helix Biased, Ultra-Short Glucagon-like Peptide-1 Receptor Agonists.

Jonathon R Sawyer, Joseph A Audie, Jon Swanson, David Diller, Solimar Santiago, Valentin K Gribkoff, Allison Ackerman, Victor J Hruby, Gianpaolo Gobbo, Michael A Bellucci and 3 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecules (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. Review
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.

Jonathon R SawyerResolute Bio, 48 Dunham Rd., Suite 5400, Beverly, MA 01915, USA.
Joseph A AudieEudoxia Life Sciences, 520 Squire Hill Rd., Cheshire, CT 06410, USA.
Jon SwansonEudoxia Life Sciences, 520 Squire Hill Rd., Cheshire, CT 06410, USA.ORCID 0000-0003-3330-7271
David DillerEudoxia Life Sciences, 520 Squire Hill Rd., Cheshire, CT 06410, USA.
Solimar SantiagoResolute Bio, 48 Dunham Rd., Suite 5400, Beverly, MA 01915, USA.
Valentin K GribkoffResolute Bio, 48 Dunham Rd., Suite 5400, Beverly, MA 01915, USA.
Allison AckermanResolute Bio, 48 Dunham Rd., Suite 5400, Beverly, MA 01915, USA.
Victor J HrubyDepartment of Chemistry and Biochemistry, The University of Arizona, 1306 E. University Blvd, Tucson, AZ 85721, USA.
Gianpaolo GobboXtalPi US, XtalPi Inc., 245 Main Street, Cambridge, MA 02142, USA.ORCID 0000-0002-8294-6152
Michael A BellucciXtalPi US, XtalPi Inc., 245 Main Street, Cambridge, MA 02142, USA.
William A GlauserXtalPi US, XtalPi Inc., 245 Main Street, Cambridge, MA 02142, USA.
Brad L PenteluteResolute Bio, 48 Dunham Rd., Suite 5400, Beverly, MA 01915, USA.
Tomi K SawyerResolute Bio, 48 Dunham Rd., Suite 5400, Beverly, MA 01915, USA.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A systematic structure-activity and computational modeling analysis of a series of glucagon-like peptide-1 receptor (GLP-1R) agonists based upon an ultra-short GLP-1 peptide, H-His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Bip-Bip-NH2, was conducted. This highly potent 11-mer peptide led to a deeper understanding of the α-helical bias of strategic α-methylation within the linear parent template as well as optimization of GLP-1R agonist potency by 1000-fold. These data were correlated with previously reported co-structures of both full-length GLP-1 analogs and progenitor N-terminal GLP-1 fragment analogs related to such ultra-short GLP-1R agonist peptides. Furthermore, the development of a quantitative structure-activity relationship (QSAR) model to analyze these findings is described in this study.

Indexed as

Drug DesignGlucagon-Like Peptide 1Glucagon-Like Peptide-1 Receptor AgonistsPeptidesComputer SimulationGlucagon-Like Peptide-1 ReceptorHumansModels, MolecularProtein Conformation, alpha-HelicalQuantitative Structure-Activity RelationshipStructure-Activity RelationshipGlucagon-Like Peptide 1Glucagon-Like Peptide-1 ReceptorGlucagon-Like Peptide-1 Receptor AgonistsPeptides2-amino-isobutyric acid (Aib)Cα-methylationglucagon-like peptide-1 (GLP-1)p-phenyl-phenylalanine (Bip)quantitative structure–activity relationship (QSAR)structure–activity relationship (SAR)structure-based designα-methyl-phenylalanine [2-F] (α-MePhe[2-F])α-methyl-phenylalanine (α-MePhe)

Identifiers

PMID39795070
PMCPMC11721672

What Socratic holds

Textmetadata
LicenceCC BY
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 Socratic graph.