Insights into GLP-1 Receptor Activation with a Nonpeptide Agonist
نویسندگان
چکیده
منابع مشابه
Expression and Characterization of a Potent Long-Acting GLP-1 Receptor Agonist, GLP-1-IgG2σ-Fc
Human GLP-1 (glucagon-like peptide-1) can produce a remarkable improvement in glycemic control in patients with type 2 diabetes. However, its clinical benefits are limited by its short half-life, which is less than 2 min because of its small size and rapid enzymatic inactivation by dipeptidyl peptidase IV. We engineered GLP-1-IgG2σ-Fc, a 68-kDa fusion protein linking a variant human GLP-1 (A8G/...
متن کاملNovel GLP-1 Fusion Chimera as Potent Long Acting GLP-1 Receptor Agonist
GLP-1 has a variety of anti-diabetic effects. However, native GLP-1 is not suitable for therapy of diabetes due to its short half-life (t1/2<2 min). To circumvent this, we developed a long-lasting GLP-1 receptor agonist by the fusion of GLP-1 with human IgG2 Fc (GLP-1/hIgG2). ELISA-based receptor binding assay demonstrated that GLP-1/hIgG2 had high binding affinity to the GLP-1R in INS-1 cells ...
متن کاملGLP-1 Receptor Agonist and Non-Alcoholic Fatty Liver Disease
Non-alcoholic fatty liver disease (NAFLD), one of the most common liver diseases, is caused by the disruption of hepatic lipid homeostasis. It is associated with insulin resistance as seen in type 2 diabetes mellitus. Glucagon-like peptide-1 (GLP-1) is an incretin that increases insulin sensitivity and aids glucose metabolism. In recent in vivo and in vitro studies, GLP-1 presents a novel thera...
متن کاملGLP-1 Receptor Agonist Effects on Normal and Neoplastic Pancreata
In this issue of Diabetes, two articles describe preclinical studies evaluating the effects of chronic glucagon-like peptide 1 (GLP-1)–based therapy on development of pancreatitis and pancreatic neoplasia (1,2). These studies were performed in light of recent case reports and a case-control study suggesting that diabetic individuals using sitagliptin or exenatide have a several-fold increased l...
متن کاملBrain activation following peripheral administration of the GLP-1 receptor agonist exendin-4.
The aim of our study was to investigate the anorectic and brain stimulatory effects of various doses of exendin-4 (Ex-4) and to investigate the role of the vagus nerve in Ex-4-induced brain activation. A dose-related increase in c-fos mRNA expression was observed following Ex-4 administration (0.155-15.5 μg/kg). Doses of Ex-4 that caused anorexia without aversive effects (0.155, 0.775 μg/kg) in...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Biochemistry
سال: 2020
ISSN: 0006-2960,1520-4995
DOI: 10.1021/acs.biochem.0c00180