Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC(50)=18nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC(50)=2.6nM), selective, and efficacious in an oral glucose tolerance test in mice. It was selected for extensive preclinical development as a potential back-up candidate to sitagliptin.
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http://dx.doi.org/10.1016/j.bmcl.2006.09.099 | DOI Listing |
Clin Kidney J
January 2025
Department of Nephrology-Hypertension, Antwerp University Hospital, Edegem, Belgium.
Background: Although post-transplant diabetes mellitus (PTDM) is a common complication after kidney transplantation, there are few data on prevention, optimal screening, and treatment strategies.
Methods: The European Renal Association's DESCARTES working group distributed a web-based survey to European transplant centres to gather information on risk assessment, screening procedures, and management practices for preventing and treating PTDM in kidney transplant recipients.
Results: Answers were obtained from 121/241 transplant centres (50%) across 15 European countries.
Fed Pract
November 2024
Aptive Resources, Alexandria, Virginia.
Background: In May 2020, the US Food and Drug Administration (FDA) asked 5 pharmaceutical companies to voluntarily recall some formulations of metformin due to contamination. This observational study sought to provide insight changes in hemoglobin A (HbA) levels when veterans switched to alternative antihyperglycemic agents following the recall.
Methods: This study included veterans aged ≥ 18 years with type 2 diabetes who were receiving health care from Veterans Integrated Service Network 6 and had an active metformin sustained-action (SA) prescription as of June 1, 2020.
Biochim Biophys Acta Mol Basis Dis
January 2025
Department of Healthcare Administration, Asia University, 40454 Taichung, Taiwan. Electronic address:
Introduction: Dipeptidyl peptidase-4 is known to be involved in the progression of several fibrogenic diseases, but its association with oral submucous fibrosis remains unclear. This study aims to ascertain whether dipeptidyl peptidase-4 plays a role in the pathogenesis of arecoline-induced oral submucous fibrosis.
Methods: We assessed the expression of dipeptidyl peptidase-4 in arecoline-treated epithelial cells and the exosomes derived from cells.
Nat Med
January 2025
Clinical Epidemiology Center, Research and Development Service, VA St. Louis Health Care System, St. Louis, MO, USA.
Glucagon-like peptide 1 receptor agonists (GLP-1RAs) are increasingly being used to treat diabetes and obesity. However, their effectiveness and risks have not yet been systematically evaluated in a comprehensive set of possible health outcomes. Here, we used the US Department of Veterans Affairs databases to build a cohort of people with diabetes who initiated GLP-1RA (n = 215,970) and compared them to those who initiated sulfonylureas (n = 159,465), dipeptidyl peptidase 4 (DPP4) inhibitors (n = 117,989) or sodium-glucose cotransporter-2 (SGLT2) inhibitors (n = 258,614), a control group composed of an equal proportion of individuals initiating sulfonylureas, DPP4 inhibitors and SGLT2 inhibitors (n = 536,068), and a control group of 1,203,097 individuals who continued use of non-GLP-1RA antihyperglycemics (usual care).
View Article and Find Full Text PDFJ Vet Intern Med
January 2025
Department of Small Animal Clinical Sciences, Western College of Veterinary Medicine, University of Saskatchewan, Saskatoon, Saskatchewan, Canada.
Background: The pathophysiology of polyuria and polydipsia secondary to exogenous glucocorticoid excess is incompletely understood.
Objective: Investigate plasma AVP (pAVP) and serum CoP (sCoP) concentrations in healthy dogs before, during, and after abrupt discontinuation of a long-term course of orally administered prednisolone.
Animals: Eight healthy neutered young adult research Beagles.
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