Microwave-assisted solid phase synthesis, PEGylation, and biological activity studies of glucagon-like peptide-1(7–36) amide

Bioorganic & Medicinal Chemistry
2008.0

Abstract

The insulinotropic hormone glucagon-like peptide-1 (GLP-1) is rapidly inactivated in the body. In order to improve its stability, we replaced the enzymatic hydrolyzation position Ala(8)with Gly and replaced Ala(30) with Cys firstly. Then the modified peptide was further PEGylated at thiol group of Cys(30). Biological activity studies showed that the resulting mPEG-MAL-Gly(8)-Cys(30)-GLP-1(7-36)-NH(2) exhibited long-lasting effect while maintaining moderate glucose-lowering activity.

Knowledge Graph

Similar Paper

Microwave-assisted solid phase synthesis, PEGylation, and biological activity studies of glucagon-like peptide-1(7–36) amide
Bioorganic & Medicinal Chemistry 2008.0
Synthesis and biological evaluation of glucagon-like peptide-1 analogs with the C-terminal helix 3 of albumin-binding domain 3
Bioorganic & Medicinal Chemistry 2022.0
Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7–36) analog
Bioorganic & Medicinal Chemistry Letters 2004.0
Influence of Selective Fluorination on the Biological Activity and Proteolytic Stability of Glucagon-like Peptide-1
Journal of Medicinal Chemistry 2008.0
Design, Synthesis, and Biological Activity of Novel Dicoumarol Glucagon-like Peptide 1 Conjugates
Journal of Medicinal Chemistry 2013.0
A General Method for Making Peptide Therapeutics Resistant to Serine Protease Degradation: Application to Dipeptidyl Peptidase IV Substrates
Journal of Medicinal Chemistry 2013.0
Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide
Journal of Medicinal Chemistry 2015.0
Peptide Half-Life Extension: Divalent, Small-Molecule Albumin Interactions Direct the Systemic Properties of Glucagon-Like Peptide 1 (GLP-1) Analogues
Journal of Medicinal Chemistry 2017.0
Novel lipid side chain modified exenatide analogs emerged prolonged glucoregulatory activity and potential body weight management properties
Bioorganic & Medicinal Chemistry 2019.0
Improving Metabolic Stability by Glycosylation: Bifunctional Peptide Derivatives That Are Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists
Journal of Medicinal Chemistry 2009.0