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diagnostics
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the activity of DPPIV measured in the tear fluid might serve as an indicator of early corneal disorders, e.g.corneal vascularization related to contact lens wear
drug development
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a three-dimensional pharmacophore model is a useful tool for designing novel DPP-IV inhibitors
food industry
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use of enzyme for degradation of food-derived opiods from milk, soybean, wheat
analysis
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the enzyme can be used for peptide sequence analysis
analysis
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surface marker for a subpopulation of human T-lymphocytes
analysis
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the enzyme is a marker for T lymphocytes
analysis
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significant levels of enzyme activity are present in commercial human serum albumin. This activity is abolished using a specific DPP-IV inhibitor. Fully 70 to 80% DPP-IV activity remains at 60°C compared with the 37°C incubate. No DPP-IV activity is present in recombinant human serum albumin, suggesting that DPP-IV activity is present only in serum albumin produced using the Cohn fractionation process. DPP-IV activity contributes to the formation of aspartate-alanine diketopiperazine, a known immunomodulatory molecule from the N terminus of human albumin, could account for some of the clinical effects of commercial human serum albumin
analysis
method for specific recognition and imaging for DPP IV in living cells by by coupling the inhibitor alogliptin to a carboxyl-modified fluorophore. The probe shows photostability and good biocompatibility. Alogliptin interacts with residues Glu206, Arg125 and Tyr631
medicine
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enzyme is a potential target for treatment of metabolic diseases
medicine
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enzyme is an important target in therapy of cancer
medicine
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specific inhibition of the enzyme shows efficacy in the treatment of type 2 diabetes
medicine
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specific inhibition of the enzyme shows efficacy in the treatment of type 2 diabetes
medicine
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specific inhibition of the enzyme shows efficacy in the treatment of type 2 diabetes
medicine
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(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide is a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
medicine
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dipeptidyl peptidase IV inhibitors are a promising new therapeutic approach for the management of type 2 diabetes
medicine
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inhibition of DPP-IV can be an effective approach to treat type 2 diabetes mellitus by potentiating insulin secretion. 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, i.e. KR-62436, could be good lead compound for further development as a new anti-diabetic agent
medicine
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inhibition of DPP-IV can be an effective approach to treat type 2 diabetes mellitus by potentiating insulin secretion. 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, i.e. KR-62436, could be good lead compound for further development as a new anti-diabetic agent
medicine
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inhibition of DPP-IV can be an effective approach to treat type 2 diabetes mellitus by potentiating insulin secretion. 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, i.e. KR-62436, could be good lead compound for further development as a new anti-diabetic agent
medicine
(2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridinecarboxylic acid (i. e. ABT-279) is a very potent, selective, effective, and well-tolerated inhibitor useful for the treatment of diabetes
medicine
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione is a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. Potential for once-daily treatment of type 2 diabetics
medicine
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a DPP-IV inhibitor (3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate) in combination with glybenclamide or nateglinide may be a promising option for the treatment of type 2 diabetes, and particularly, for controlling postprandial hyperglycemia in the clinic
medicine
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a DPP-IV inhibitor (3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate) in combination with glybenclamide or nateglinide may be a promising option for the treatment of type 2 diabetes, and particularly, for controlling postprandial hyperglycemia in the clinic
medicine
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addition of sitagliptin 50 mg b.i.d. to ongoing metformin therapy improves 24-h glycaemic control and beta-cell function, and is generally well tolerated in patients with type 2 diabetes
medicine
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application of dipeptidyl peptidase IV inhibitors in managing type 2 diabetes mellitus
medicine
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both sitagliptin and vildagliptin improve metabolic control in type-2 diabetes, both in monotherapy and in combination with metformin and thiazolidinediones. DPP-4 inhibition is safe and well tolerated, the risk of hypoglycaemia is minimal, an DPP-4 inhibition is body-weight neutral. DPP-4 inhibition is suggested to be a first-line treatment of type-2 diabetes, particularly in its early stages in combination with metformin
medicine
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CD26 inhibition may represent a novel approach to increasing the efficacy and success of hematopoietic stem cell/hematopoietic progenitor cell transplantation, especially under conditions of limiting donor cell yield
medicine
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CD26 inhibition may represent a novel approach to increasing the efficacy and success of hematopoietic stem cell/hematopoietic progenitor cell transplantation, especially under conditions of limiting donor cell yield
medicine
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CD26 is an appropriate molecular target for renal cell carcinoma therapy. Anti-CD26 mAb treatment leads to loss of tumorigenicity. The potent antitumor effect of anti-CD26 mAb may be used in the future as novel therapeutic approaches against various CD26-positive malignancies, including renal cell carcinoma
medicine
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CD26 on donor human cord blood cells is a negative regulator of the engraftment of long-term repopulating cells. CD26 inhibitor treatment of donor cells prior to transplant has the ability to improve long-term engraftment
medicine
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CD26/DP IV is a nonredundant inhibitory receptor controlling T cell activation and Th1-mediated autoimmunity, and may have important therapeutic implications for the treatment of autoimmune CNS disease
medicine
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co-administration of the dipeptidyl peptidase-4 inhibitor sitagliptin and metformin is well tolerated in patients with type 2 diabetes and does not alter the steady-state pharmacokinetics of either agent
medicine
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coadministration of a single oral CSA dose with a single dose of sitagliptin modestly increases maximal plasma concentration of sitagliptin
medicine
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combination of DPP IV inhibitor with low dose of thiazolidinedione can interact synergistically to represent a therapeutic advantage for the clinical treatment of type 2 diabetes without the adverse effects of haemodilution and weight gain associated with thiazolidinediones
medicine
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combined action of DP IV and aminopeptidase N inhibitors markedly increases TGF-beta1 production associated with the observed immunosuppressive effects. In vivo, targeting both DP IV and aminopeptidase N leads to a potent treatment of experimental autoimmune encephalomyelitis, an animal model of multiple sclerosis
medicine
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dipeptidyl peptidase-4 inhibitor is approved in the United States for the treatment of type 2 diabetes. The absolute bioavailability of sitagliptin final market image tablets is approximately 87%. Food does not affect the pharmacokinetics of sitagliptin and therefore can be administered without regard to food generally well tolerated when administered orally or intravenously
medicine
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dipeptidyl peptidase-IV inhibitors can restore glucose homeostasis in type 2 diabetics via incretin enhancement
medicine
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DPP-4 inhibition increases active glucagon-like peptide 1 levels and improves glucose tolerance and islet function with improved islet topography in mice with a beta-cellspecific overexpression of human islet amyloid peptide. These findings support the potential value of DPP-4 inhibition in the treatment of diabetes with the potential of normalizing islet function
medicine
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DPP-4 inhibition sufficient to double postprandial glucogon-like peptide 1 and lower glucose concentrations in people with type 2 diabetes does not alter gastric emptying or the rate of systemic appearance of ingested glucose
medicine
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DPP-4 inhibitor therapy in the treatment of type 2 diabetes
medicine
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DPP-4 inhibitors and their potential role in the management of type 2 diabetes
medicine
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DPP-4 inhibitors are antidiabetogenic drugs, that are effective as monotherapy in patients inadequately controlled with diet and exercise and as add-on therapy in combination with metformin, thiazolidinediones, and insulin. The DPP-4 inhibitors are well tolerated, carry a low risk of producing hypoglycemia, and are weight-neutral
medicine
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DPP-4 inhibitors are effective agents for achieving blood glucose control
medicine
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DPP-4 inhibitors as therapy for type 2 diabetes
medicine
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DPP-4 inhibitors effectively stimulate insulin secretion, suppress glucagon release, and improve glucose control in patients with type 2 diabetes. These agents are well tolerated and have a low incidence of adverse effects
medicine
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DPP-IV inhibitors appear to have excellent therapeutic potential in the management of type 2 diabetes as monotherapy or in combination with existing agents, such as metformin. Their pharmacokinetic and pharmacodynamic profiles support once-daily dosing, with sustainable reductions in glycosylated hemoglobin levels and relatively few adverse effects
medicine
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DPP-IV inhibitors are potentially important therapies in diabetes
medicine
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DPP-IV inhibitors in treatment of type 2 diabetes
medicine
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DPP-IV inhibitors may have more consistent efficacy to reduce postprandial hyperglycemia, independent of the types of carbohydrate contained in a meal. The combination of a DPP-IV inhibitor and an alpha-glucosidase inhibitor is expected to be a promising option for lowering postprandial hyperglycemia
medicine
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DPP-IV is a target for the treatment of type 2 diabetes. The inhibitors vildagliptin and saxagliptin are well tolerated and reduce blood glucose and HbA1c levels in diabetic patients
medicine
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environmental or genetic factors that reduce dipeptidyl peptidase IV activity may predispose individuals to angioedema
medicine
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functional role of dipeptidyl peptidase IV and aminopeptidase N in the sebaceous gland apparatus and for their inhibitors, used alone or in combination, as substances possibly affecting acne pathogenesis in a therapeutic manner
medicine
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genetic or environmental factors that decrease DPPIV activity might increase the risk of angiotensin-converting enzyme inhibitor-associated angioedema
medicine
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glucagon-like peptide-1-based therapy is a treatment for type 2 diabetes. It is executed either by GLP-1 mimetics or by dipeptidyl peptidase-IV inhibitors. In type 2 diabetes, the two strategies reduce hemoglobin A1c by 0.6% to 1.1% from baseline levels of 7.7% to 8.5%. They are efficient both in monotherapy and in combination with metformin or thiazolidinediones. Both treatments are well tolerated with low risk of hypoglycemia
medicine
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imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabete, pharmacokinetic properties
medicine
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in a 24-week study, sitagliptin 100 mg once daily added to ongoing pioglitazone therapy is effective and well tolerated in these patients with type 2 diabetes who had not achieved adequate glycemic control with pioglitazone alone
medicine
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in genetically susceptible animals, inhibition of DPP IV increases arterial blood pressure via Y1 receptors when elevated blood pressure is reduced with antihypertensive drugs provided that the sympathetic nervous system is functional
medicine
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in patients with type 2 diabetes, near maximal glucose-lowering efficacy of sitagliptin after single oral doses is associated with inhibition of plasma DPP-4 activity of 80% or greater, corresponding to a plasma sitagliptin concentration of 100 nM or greater, and an augmentation of active glucagon-like peptide-1 and glucose-dependent insulinotropic peptide levels of 2fold or higher after an oral glucose tolerance test
medicine
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in pre-diabetic subjects, a 12-week treatment with vildagliptin markedly increases postmeal levels of active glucagon-like peptide 1 and gastric inhibitory polypeptide, improves both alpha- and beta-cell function, decreases postprandial hyperglycemia and decreases A1C levels. Vildagliptin is well tolerated and weight neutral and does not cause hypoglycemia
medicine
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inhibition of CD26 may be one way to enhance engraftment of limiting numbers of stem cells during cord blood transplantation
medicine
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inhibition of dipeptidylpeptidase IV activity as a therapy of type 2 diabetes
medicine
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major clinical trials with DPP-IV inhibitors as monotherapy and as add-on therapy in patients with type 2 diabetes. The magnitude of HbA1c reduction with DPP-IV inhibitors depends upon the pretreatment HbA1c values, but there seems to be no change in body weight, and very low rates of hypoglycaemia and gastrointestinal disturbance with these agents. DPP-IV inhibitors represent a major class of oral antidiabetic drug and their metabolic profile offers a number of unique clinical advantages for the management of type 2 diabetes
medicine
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metformin decreases the plasma DPP IV activity, limiting the inactivation of exogenously administered GLP-1 and improving glycaemic control
medicine
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monotherapy with vildagliptin is well tolerated and improves glycemic control in diet-treated subjects with type 2 diabetes
medicine
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oral dipeptidyl peptidase-4 inhibitors may prove valuable in the treatment of diabetes, given their effectiveness in reducing glycated hemoglobin with neutral weight effects and without the adverse events associated with other agents. Dipeptidyl peptidase-4 inhibitors appear to improve islet function and may modify the course of diabetes
medicine
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pharmacokinetic and pharmacodynamic assessments of the dipeptidyl peptidase-4 inhibitor PHX1149, double-blind, placebo-controlled, single- and multiple-dose studies in healthy subjects
medicine
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pituitary adenylate cyclase-activating polypeptide (PACAP) is a neuropeptide with promising therapeutic applications for the treatment of several pathophysiological states related to neurodegenerative diseases. However, its use for therapeutic applications is actually limited by its restricted bioavailability and rapid degradation. N-terminal modifications confer resistance to dipeptidyl peptidase IV, a major proteolytic process involved in PACAP degradation
medicine
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possible use of nateglindide in combination with incretin hormones for type 2 diabetes therapy. The use of nateglinide as a prandial insulin-releasing agent may partly rely on inhibition of degradation of glucagon-lioke peptide-1 as well as beta-cell K(ATP) channel inhibition
medicine
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potential treatment of type 2 diabetes with the short-acting dipeptidyl peptidase IV inhibitor PSN-9301, drug evaluation
medicine
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pre-clinical and clinical studies on DPP-IV inhibitors demonstrate significant potential for their application as therapeutic agents in the managment of type 2 diabetes
medicine
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sitagliptin is a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Use of sitagliptin as adjunct therapy to sulfonylureas and metformin. An advantage of sitagliptin use is that it appears to be free from the adverse effects of weight gain and hypoglycemia that are associated with currently available treatments
medicine
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sitagliptin is a highly selective DPP-4 inhibitor for the treatment of type 2 diabetes
medicine
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sitagliptin is a selective DPP-4 inhibitor that enhances intact incretin levels and improves 24-h glycemic control in patients with type 2 diabetes
medicine
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sitagliptin is one-daily, orally active, potent and selective DPP-4 inhibitor, which reduces both fasting and postprandial glucose levels and improves summary measures of beta-cell function to produce clinically meaningful reductions in HbA1c concentrations. Efficiacy as both a monotherapy and in combination with merformin or pioglitazone, without causing weight gain
medicine
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sitagliptin significantly improves glycaemic control and is well tolerated in patients with type 2 diabetes mellitus who have inadequate glycaemic control on exercise and diet
medicine
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the addition of sitagliptin compared with glipizide provides similar HbA1c-lowering efficacy over 52 weeks in patients with type 2 diabetes on ongoing metformin therapy. Sitagliptin is generally well tolerated, with a lower risk of hypoglycaemia relative to glipizide and with weight loss compared with weight gain with glipizide
medicine
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the dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients
medicine
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the dipeptidyl peptidase-IV inhibitor vildagliptin improves glycemic control in patients with type 2 diabetes by increasing alpha and beta-cell responsiveness to glucose. Co-administration of warfarin (a vitamin K antagonist widely used for long-term prevention of thrombosis) does not alter the pharmacokinetics of vildagliptin
medicine
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the DPP-4 inhibitor sitagliptin in diabetes therapy. Sitagliptin is effective, well tolerated and safe in clinical studies. Sitagliptin es effective in monotherapy and combination therapieswith metformin or glitazones. Sitagliptin does not show an increased incidence of hypoglycemic events
medicine
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the DPP-4 inhibitor sitagliptin is effective in treatment of type 2 diabetes. Overview of the mechanisms of action, pharmacology and clinical trial results of sitagliptin. DPP-4 inhibitors could be used in prediabetic stages and the very early stages of diabetes to slow or prevent the progression of type 2 diabetes
medicine
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the oral dipeptidyl peptidase 4 inhibitors vildagliptin, sitagliptin, and saxagliptin are efficious both alone and in association with other oral anti-diabetic agents and may be administered in a single daily dose. They have substantial advantages with respect to other anti-diabetic drugs, since they involve a low risk of hypoglycemia and do not affect body weight
medicine
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the pharmacokinetics of rosiglitazone will not be altered when coadministered with sitagliptin in patients with type 2 diabetes
medicine
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the review focuses mainly on the preclinical studies underlying the development DPP IV inhibitors appropriate for diabetes therapy and their proposed mode of action, and summarized the clinical experience to date
medicine
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therapy for type 2 diabetes mellitus with dipeptidyl peptridase-IV inhibitors
medicine
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there is no significant difference in exposure to vildagliptin in patients with mild, moderate or severe hepatic impairment. Therefore, no dose adjustment of vildagliptin is necessary in patients with hepatic impairment
medicine
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use of DPPIV inhibitors could increase the risk of promoting an already existing intestinal tumour and may support the potential of colon cancer cells to metastasize
medicine
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vildagliptin is a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. No adjustment in dosage based on pharmacokinetic considerations is required should vildagliptin be coadministered with amlodipine, valsartan, or ramipril in patients with type 2 diabetes and hypertension
medicine
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vildagliptin is a DPP-4 inhibitor with pancreatic islet enhancement activity for treatment of patients with type 2 diabetes
medicine
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vildagliptin is a novel antidiabetic agent that is an orally active, potent, and selective inhibitor of dipeptidyl peptidase IV, the enzyme responsible for degradation of the incretin hormones. No dose adjustment is necessary when vildagliptin and digoxin are coadministered
medicine
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vildagliptin is a potent and selective dipeptidyl peptidase IV inhibitor in development for the treatment of type 2 diabetes that improves glycemic control by enhancing alpha- and beta-cell responsiveness to glucose. Vildagliptin displays approximately dose-proportional pharmacokinetics over the 25-mg to 200-mg dose range, and administration with food has no clinically relevant effect on vildagliptin pharmacokinetics
medicine
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coadministration of DPP-4 inhibitor vildagliptin with either glyburide or pioglitazone in patients with diabetes type 2 improves postprandial glycemic control
medicine
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dipeptidyl peptidase IV inhibitors can reduce fat infiltration in the liver and thus be a potential treatment for non-alcoholic fatty liver disease
medicine
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dipeptidyl peptidase IV is a target for the treatment of type 2 diabetes mellitus
medicine
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DPP-4 inhibition augments postprandial lipid mobilization and oxidation and increases endogenous glucagon-like peptide 1 activity, resulting in improved glycemic control in patients with type 2 diabetes mellitus
medicine
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DPP-4 inhibition in combination with metformin is an efficient, safe and tolerable combination therapy for type 2 diabetes
medicine
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DPP-4 inhibition is an oral therapy for type 2 diabetes
medicine
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DPP-IV is a target for the treatment of type 2 diabetes
medicine
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DPP-IV is a target for the treatment of type 2 diabetes
medicine
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DPP-IV is a target for the treatment of type 2 diabetes
medicine
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concurrent measurement of adenosine deaminase and dipeptidyl peptidase IV can aid in diagnosing tuberculous pleural effusion
medicine
DPIV is a type 2 diabetes therapeutic target
medicine
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DPPIV expression may be an in vivo marker of tumor sensitivity to paclitaxel treatment
medicine
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DPPIV/CD26 demonstrate potential as biomarkers for chronic fatigue syndrome
medicine
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the DPP-IV activity decreases in mucopolysacharidoses I patients undergoing enzyme replacement therapy, indicating that it can be a useful biomarker for monitoring the efficacy of treatment in mucopolysacharidoses disease
medicine
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dipeptidyl peptidase IV functions as a chemorepellent of human neutrophils
medicine
dipeptidyl peptidase IV might be responsible for the shallow implantation of the placenta due to its inhibition of the invading ability of extravillous trophoblasts, causing preeclampsia at later stage of pregnancy
medicine
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enzyme is able to truncate the commercial amyloid beta40 and amyloid beta42 peptides, to hinder the fibril formation by them and to participate in the disaggregation of preformed fibrils of these peptides. Dipeptidyl peptidase IV hinders the peptide aggregation/fibrillation during 3-4 days incubation in 20 mM phosphate buffer, pH 7.4, 37°C by 50-80%. In the presence of dipeptidyl peptidase IV, the preformed fibrils are disaggregated by 30-40%
medicine
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in a murine model of acute respiratory distress syndrome, aspirated bleomycin induces a significant increase in the number of neutrophils in the lungs after 3 d. Oropharyngeal aspiration of dipeptidyl peptidase IV inhibits the bleomycin-induced accumulation of mouse neutrophils
medicine
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mRNA expression in ipsilateral and contralateral cortices. At day 3 post-ischemia, dipeptidyl peptidase IV, 8 and aminopeptidase N are identified in activated microglia and macrophages in the ipsilateral cortex. Seven days post artery occlusion, dipeptidyl peptidase IV immunoreactivity is found in the perikarya of surviving cortical neurons of the ipsilateral hemisphere. At the same time point, dipeptidyl peptidase IV, 8 and aminopeptidase N are targeted in astroglial cells. Total dipeptidyl peptidase IV, 8 and 9 activities remain constant in both hemispheres until day 3 post experimental ischemia, but are increased to 165% in the ipsilateral cortex at day 7. Dipeptidyl peptidase II and aminopeptidase N are up-regulated ipsilaterally from 6 h to 7 days post ischemia. IPC1755, a non-selective protease inhibitor, reveals a significant reduction of cortical lesions after transient cerebral ischemia
medicine
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significant levels of enzyme activity are present in commercial human serum albumin. This activity is abolished using a specific DPP-IV inhibitor. Fully 70 to 80% DPP-IV activity remains at 60°C compared with the 37°C incubate. No DPP-IV activity is present in recombinant human serum albumin, suggesting that DPP-IV activity is present only in serum albumin produced using the Cohn fractionation process. DPP-IV activity contributes to the formation of aspartate-alanine diketopiperazine, a known immunomodulatory molecule from the N terminus of human albumin, could account for some of the clinical effects of commercial human serum albumin
medicine
association between peptidases and aggressive and externalizing behaviors. DPP-IV is significantly and positively associated with the Child Behavior Checklist attention problems, aggressive and externalizing behavior subscales. There is a negative correlation between the peptidase and age and Tanner stage. DPP-IV is associated with alpha2-globulin (positively) and IgG3 (inversely) levels
pharmacology
enzyme is a target for drug design
pharmacology
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target for development of selective inhibitors for control of the enzyme's biological function
veterinary medicine
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inhibition of intragraft DPP IV enzymatic activity significantly reduces ischemia/reperfusion-associated pulmonary injury, allowing for successful transplantation after 18 h of ischemia
veterinary medicine
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inhibiting intragraft DPP IV enzymatic activity in a rat single-lung transplantation model abolishes ischemia/reperfusion injury after extended ischemia