ArticlePloS one2013
Stimulating β-cell regeneration by combining a GPR119 agonist with a DPP-IV inhibitor.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 38 citations in OpenAlex.
- Use of Sitagliptin With Closed-Loop Technology to Decrease Postprandial Blood Glucose in Type 1 Diabetes.Journal of diabetes science and technology · 2017Trial
- GPCRs involved in metabolic diseases: pharmacotherapeutic development updates.Acta pharmacologica Sinica · 2024Review
- Multi-Target Approaches in Metabolic Syndrome.Frontiers in pharmacology · 2020Review
- The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo.Scientific reports · 2017Article
- Incretin Therapies Do Not Expand β-Cell Mass or Alter Pancreatic Histology in Young Male Mice.Endocrinology · 2017Article
- Cannabinoids Modulate Neuronal Activity and Cancer by CB1 and CB2 Receptor-Independent Mechanisms.Frontiers in pharmacology · 2017Review
- Article
- A Comprehensive Review of Novel Drug-Disease Models in Diabetes Drug Development.Clinical pharmacokinetics · 2016Review
- An Update on the Effect of Incretin-Based Therapies on β-Cell Function and Mass.Diabetes & metabolism journal · 2016Review
- Activation of GPR119 Stimulates Human β-Cell Replication and Neogenesis in Humanized Mice with Functional Human Islets.Journal of diabetes research · 2016Article
- Combination immunotherapies for type 1 diabetes mellitus.Nature reviews. Endocrinology · 2015Review
- Recent progress in studies of factors that elicit pancreatic β-cell expansion.Protein & cell · 2015Review
- N-stearoylethanolamine restores pancreas lipid composition in obesity-induced insulin resistant rats.Lipids · 2015Article
- Pharmacology, physiology, and mechanisms of action of dipeptidyl peptidase-4 inhibitors.Endocrine reviews · 2014Review
- Gastrointestinal hormonal responses on GPR119 activation in lean and diseased rodent models of type 2 diabetes.International journal of obesity (2005) · 2014Article
- Human β-cell regeneration: progress, hurdles, and controversy.Current opinion in endocrinology, diabetes, and obesity · 2014Review
- Combining MK626, a novel DPP-4 inhibitor, and low-dose monoclonal CD3 antibody for stable remission of new-onset diabetes in mice.PloS one · 2014Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundActivating G-protein coupled receptor 119 (GPR119) by its agonists can stimulate glucagon like peptide-1 (GLP-1) release. GLP-1 is rapidly degraded and inactivated by dipeptidylpeptidase-IV (DPP-IV). We studied the efficiency of combining PSN632408, a GPR119 agonist, with sitagliptin, a DPP-IV inhibitor, on β-cell regeneration in diabetic mice. MATERIALS &
methodsDiabetes in C57BL/6 mice was induced by streptozotocin. PSN632408 and sitagliptin alone or in combination were administered to diabetic mice for 7 weeks along with BrdU daily. Nonfasting blood glucose levels were monitored. After treatment, oral glucose tolerance test (OGTT), plasma active GLP-1 levels, β-cell mass along with α- and β-cell replication, and β-cell neogenesis were evaluated.
resultsNormoglycemia was not achieved in vehicle-treated mice. By contrast, 32% (6 of 19) of PSN632408-treated diabetic mice, 36% (5 of 14) sitagliptin-treated diabetic mice, and 59% (13 of 22) diabetic mice treated with PSN632408 and sitagliptin combination achieved normoglycemia after 7 weeks treatment. Combination therapy significantly increased plasma active GLP-1 levels, improved glucose clearance, stimulated both α- and β-cell replication, and augmented β-cell mass. Furthermore, treatment with combination therapy induced β-cell neogenesis from pancreatic duct-derived cells.
conclusionOur results demonstrate that combining a GPR119 agonist with a DPP-IV inhibitor may offer a novel therapeutic strategy for stimulating β-cell regeneration and reversing diabetes.
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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.