Journal ArticleDOI
Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes.
James Mu,Aleksandr Petrov,George J. Eiermann,John Woods,Yun-Ping Zhou,Zhihua Li,Emanuel Zycband,Yue Feng,Lan Zhu,Ranabir Sinha Roy,Andrew D. Howard,Cai Li,Nancy A. Thornberry,Bei B. Zhang +13 more
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TLDR
Improvement in glycemic control in sitagliptin-treated mice was associated with a significant increase in glucose-dependent insulin secretion in both perfused pancreas and isolated islets, and in contrast to the lack of effect by glipizide, sitgliptin significantly restored beta and alpha cell mass as well as alpha/beta cell ratio.About:
This article is published in European Journal of Pharmacology.The article was published on 2009-11-25. It has received 128 citations till now. The article focuses on the topics: Sitagliptin Phosphate & Sitagliptin.read more
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The molecular mechanisms of pancreatic β-cell glucotoxicity: recent findings and future research directions.
TL;DR: Deciphering these molecular mechanisms of β- cell glucotoxicity is a mandatory first step toward the development of therapeutic strategies to protect β-cells and improve the functional β-cell mass in type 2 diabetes.
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Incretin action in the pancreas: Potential promise, possible perils, and pathological pitfalls
TL;DR: Recent advances and controversies in incretin hormone action in the pancreas are reviewed and established mechanisms with areas of uncertainty are contrasted and methodological challenges and pitfalls are highlighted.
Journal ArticleDOI
Generation of a Transgenic Mouse Model of Middle East Respiratory Syndrome Coronavirus Infection and Disease
Anurodh S. Agrawal,Tania Garron,Xinrong Tao,Bi Hung Peng,Maki Wakamiya,Teh Sheng Chan,Robert B. Couch,Chien Te K. Tseng +7 more
TL;DR: It is shown that transgenic mice globally expressing hCD26/DPP4 were fully permissive to MERS-CoV infection, resulting in relentless weight loss and death within days postinfection, and this new and unique transgenic mouse model will be useful for furthering knowledge of MERS pathogenesis and for the development of vaccine and treatments against MSPV.
Journal ArticleDOI
Effects of Sitagliptin Treatment on Dysmetabolism, Inflammation, and Oxidative Stress in an Animal Model of Type 2 Diabetes (ZDF Rat)
Liliana P. Ferreira,Edite Teixeira-de-Lemos,Filipa Pinto,Belmiro Parada,C. Mega,Helena Vala,Rui Pinto,Patrícia Garrido,José Sereno,Rosa Fernandes,Paulo F. Santos,Isabel Velada,Andreia Cristina de Melo,Sara Nunes,Frederico Teixeira,Flávio Reis +15 more
TL;DR: Chronic sitagliptin treatment corrected the glycaemic dysmetabolism, hypertriglyceridaemia, inflammation, and hypertension, reduced the severity of the histopathological lesions of pancreatic endocrine and exocrine tissues, together with a favourable redox status, which might be a further advantage in the management of diabetes and its proatherogenic comorbidities.
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Assessment of pancreatic β-cell function: review of methods and clinical applications.
Eugenio Cersosimo,Carolina Solis-Herrera,Michael E. Trautmann,Jaret Malloy,Curtis L Triplitt +4 more
TL;DR: This review focuses on the most widely used methods for measuring BCF within the context of insulin resistance and includes examples of their use in prediabetes and T2DM, with an emphasis in the most recent therapeutic options (dipeptidyl peptidase-4 inhibitors and glucagon-like peptide-1 receptor agonists).
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Journal ArticleDOI
The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes
TL;DR: Clinical trials with the incretin mimetic exenatide and liraglutide show reductions in fasting and postprandial glucose concentrations, and haemoglobin A1c (HbA1c) associated with weight loss, but long-term clinical studies are needed to determine the benefits of targeting the inc retin axis for the treatment of type 2 diabetes.
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Method for the Isolation of Intact Islets of Langerhans from the Rat Pancreas
Paul E. Lacy,Mery Kostianovsky +1 more
TL;DR: A simple method for the isolation of intact islets from the normal rat pancreas is described, based upon disruption of the acinar parenchyma by injecting Hanks solution into the pancreatic duct system followed by incubation of the Pancreas in collagenase.
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Exendin-4 stimulates both beta-cell replication and neogenesis, resulting in increased beta-cell mass and improved glucose tolerance in diabetic rats.
TL;DR: It is reported that exendin-4, a long-acting GLP-I agonist, stimulates both the differentiation of beta-cells from ductal progenitor cells (neogenesis) and proliferation of Beta-cells when administered to rats and holds promise as a novel therapy to stimulate beta-cell growth and differentiation when administer to diabetic individuals with reduced beta- cell mass.
Journal ArticleDOI
(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Dooseop Kim,Liping Wang,Maria G. Beconi,George J. Eiermann,Michael H. Fisher,Huaibing He,Gerard J. Hickey,Jennifer E. Kowalchick,Barbara Leiting,Kathryn A. Lyons,Frank Marsilio,Margaret E. McCann,Reshma A. Patel,Aleksandr Petrov,Giovanna Scapin,Sangita B. Patel,Ranabir Sinha Roy,Joseph K. Wu,Matthew J. Wyvratt,Bei B. Zhang,Lan Zhu,Nancy A. Thornberry,Ann E. Weber +22 more
TL;DR: A novel series of beta-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes and MK-0431, the phosphate salt of compound 1, was selected for development.
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β-Cell Failure in Diabetes and Preservation by Clinical Treatment
TL;DR: Among the interventions to preserve or "rejuvenate" beta-cells, short-term intensive insulin therapy of newly diagnosed type 2 diabetes will improve beta-cell function, usually leading to a temporary remission time and the use of antiapoptotic drugs, such as the thiazolidinediones (TZDs), and incretin mimetics and enhancers, which have demonstrated significant clinical evidence of effects on human beta- cell function.