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

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

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 understan...

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Bibliographic Details
Main Authors: 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, William A. Glauser, Brad L. Pentelute, Tomi K. Sawyer
Format: Article
Language:English
Published: MDPI AG 2024-12-01
Series:Molecules
Subjects:
glucagon-like peptide-1 (GLP-1)
Cα-methylation
<i>p</i>-phenyl-phenylalanine (Bip)
2-amino-isobutyric acid (Aib)
α-methyl-phenylalanine (α-MePhe)
α-methyl-phenylalanine [2-F] (α-MePhe[2-F])
Online Access:https://www.mdpi.com/1420-3049/30/1/12
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