Signal Peptide Optimization to Prevent N-terminal Truncation of ...
2020年8月31日 · In an attempt to develop a biosimilar version of dulaglutide, we found that up to 75% of GLP-1-Fc displayed N-terminal truncations in one or both GLP-1 arms. We proposed that the N-terminal heterogeneity was caused by mis-cleavage of signal peptide and solved this problem through signal peptide optimization.
Dulaglutide, a long-acting GLP-1 analog fused with an Fc ... - PubMed
Dulaglutide (LY-2189265) is a novel, long-acting glucagon-like peptide 1 (GLP-1) analog being developed by Eli Lilly for the treatment of type 2 diabetes mellitus (T2DM). Dulaglutide consists of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4, thereby protecting the …
Glucagon-like peptide-1 receptor: mechanisms and advances in …
2024年9月18日 · It provides an in-depth assessment of the effectiveness of GLP-1RAs across multiple body systems-including the nervous, cardiovascular, musculoskeletal, and digestive systems. This includes...
Signal Peptide Optimization to Prevent N-terminal Truncation …
2020年8月31日 · In an attempt to develop a biosimilar version of dulaglutide, we found that up to 75% of GLP-1-Fc displayed N-terminal truncations in one or both GLP-1 arms. We proposed that the N-terminal...
Long-Term Activation of Glucagon-like peptide-1 receptor by Dulaglutide …
2022年9月29日 · Dulaglutide treatment functionally attenuated cardiac remodeling and dysfunction and promoted metabolic reprogramming in diabetic mice. Furthermore, dulaglutide improved mitochondria fragmentation in myocytes, and simultaneously reinstated mitochondrial morphology and function in diabetic hearts.
Expression and Characterization of a Potent Long-Acting GLP
2021年8月11日 · GLP-1 is a glucose-dependent intestinal hypoglycemic polypeptide hormone secreted by L cells of the terminal jejunum, ileum and colon. The peptide hormone promotes glycemic-dependent insulin secretion, inhibits glucagon secretion, suppresses appetite, and stimulates pancreatic β cell proliferation and inhibits its apoptosis.
A novel GLP-1 and FGF21 dual agonist has therapeutic potential …
2021年1月7日 · In this study we optimized an FGF21 protein and presented a novel long-acting GLP-1/FGF21 dual-targeted fusion protein. This dual agonist can potently activate both GLP-1 and FGF21 receptors and in different mice models, the dual agonist shows potent anti-diabetic and anti-obesity effects.
Application of Adaptive Design Methodology in Development of a …
Dulaglutide (dula, LY2189265), a long-acting glucagon-like peptide-1 analog, is being developed to treat type 2 diabetes mellitus. To foster the development of dula, we designed a two-stage adaptive, dose-finding, inferentially seamless phase 2/3 ...
Murine immunoglobulin kappa light chain signal pep-tide (KASP) significantly improves GLP-1-Fc N-terminal integrity and homogeneity. 92.8–95.7% of GLP-1-Fc molecules directed by KASP contain intact N-terminus. The productivity of GLP-1-Fc …
Advances in GLP-1 receptor agonists for pain treatment and their …
Glucagon-like peptide-1 receptor agonists (GLP-1RAs) show substantial efficacy in regulating blood glucose levels and lipid metabolism, initially as an effective treatment for diabetes mellitus. ... At present, several GLP-1 analogs have joined the class, such as exenatide, liraglutide, dulaglutide, semaglutide and tirzepatide . Glucagon-like ...