ArticlePloS one2010
Novel GLP-1 fusion chimera as potent long acting GLP-1 receptor agonist.
Article in PloS one, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 47 citations in OpenAlex.
- Efficacy and safety of efsubaglutide alfa in individuals with type 2 diabetes (SUPER1): a randomised, double-blind, placebo-controlled, Phase IIb/III trial.Diabetologia · 2026Trial
- Efsubaglutide alfa added to metformin improves glycaemia with β-cell functional responses in type 2 diabetes: a randomised, double-blind, placebo-controlled, two-stage adaptive phase 2b/3 trial (SUPER 2).Nature communications · 2026Trial
- Diabetes Remission in Drug-Naïve Patients with Type 2 Diabetes After Efsubaglutide Alfa Treatment.Advances in therapy · 2026Trial
- Exposure-Response Analysis of Efsubaglutide Alfa in Patients with Type 2 Diabetes Treated with Metformin.Clinical pharmacokinetics · 2025Trial
- Effect of Efsubaglutide Alfa on the Pharmacokinetics of Metformin and Digoxin in Healthy Participants.Clinical pharmacokinetics · 2025Trial
- Population Pharmacokinetics of Efsubaglutide Alfa in Healthy Subjects and Subjects with Type 2 Diabetes.Clinical pharmacokinetics · 2025Trial
- Efsubaglutide Alfa: A Comprehensive Pharmacological Review.Clinical pharmacokinetics · 2026Review
- Long-acting management of diabetes and associated complications using an injectable thermosensitive hydrogel incorporating IgG-conjugated GLP-1RA.Theranostics · 2026Article
- Supaglutide alleviates hepatic steatosis in monkeys with spontaneous MASH.Diabetology & metabolic syndrome · 2024Article
- Parental sex-dependent effects of either maternal or paternal eNOS deficiency on the offspring's phenotype without transmission of the parental eNOS deficiency to the offspring.Frontiers in physiology · 2023Article
- Paternal eNOS deficiency in mice affects glucose homeostasis and liver glycogen in male offspring without inheritance of eNOS deficiency itself.Diabetologia · 2022Article
- Chimeric Claudins: A New Tool to Study Tight Junction Structure and Function.International journal of molecular sciences · 2021Article
- Novel GLP-1 Analog Supaglutide Stimulates Insulin Secretion in Mouse and Human Islet Beta-Cells and Improves Glucose Homeostasis in Diabetic Mice.Frontiers in physiology · 2019Article
- Antibody-mediated oral delivery of therapeutic DNA for type 2 diabetes mellitus.Biomaterials research · 2018Article
- GLP-1 Improves Adipocyte Insulin Sensitivity Following Induction of Endoplasmic Reticulum Stress.Frontiers in pharmacology · 2018 · on this mapArticle
- Novel GLP-1 Analog Supaglutide Reduces HFD-Induced Obesity Associated with Increased Ucp-1 in White Adipose Tissue in Mice.Frontiers in physiology · 2017Article
- Cardiovascular Benefits of Native GLP-1 and its Metabolites: An Indicator for GLP-1-Therapy Strategies.Frontiers in physiology · 2017Review
- Quantitative Impact of Plasma Clearance and Down-regulation on GLP-1 Receptor Molecular Imaging.Molecular imaging and biology · 2016Article
- Variant fatty acid-like molecules Conjugation, novel approaches for extending the stability of therapeutic peptides.Scientific reports · 2015Article
- Fusion Proteins for Half-Life Extension of Biologics as a Strategy to Make Biobetters.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy · 2015Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
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 (Kd = 13.90±1.52 nM). Upon binding, GLP-1/hIgG2 was rapidly internalized by INS-1 cells in a dynamin-dependent manner. Insulin RIA showed that GLP-1/IgG2 dose-dependently stimulated insulin secretion from INS-1 cells. Pharmacokinetic studies in CD1 mice showed that with intraperitoneal injection (i.p.), the GLP-1/hIgG2 peaked at 30 minutes in circulation and maintained a plateau for >168 h. Intraperitoneal glucose tolerance test (IPGTT) in mice showed that GLP-1/hIgG2 significantly decreased glucose excursion. Furthermore, IPGTT performed on mice one week after a single drug-injection also displayed significantly reduced glucose excursion, indicating that GLP-1/hIgG2 fusion protein has long-lasting effects on the modulation of glucose homeostasis. GLP-1/hIgG2 was found to be effective in reducing the incidence of diabetes in multiple-low-dose streptozotocin-induced type 1 diabetes in mice. Together, the long-lasting bioactive GLP-1/hIgG2 retains native GLP-1 activities and thus may serve as a potent GLP-1 receptor agonist.
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Registered trials
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 OpenQuestion graph.