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Peptidase inhibitor

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https://www.readbyqxmd.com/read/28230454/adherence-persistence-and-health-care-costs-for-patients-receiving-dipeptidyl-peptidase-4-inhibitors
#1
Karen L Rascati, Karen Worley, Yunus Meah, Damian Everhart
BACKGROUND: The dipeptidyl peptidase-4 (DPP-4) inhibitors are among the newer, yet more established, classes of diabetes medications. OBJECTIVE: To compare adherence, persistence, and health care costs among patients taking DPP-4 inhibitors. METHODS: Claims were extracted from Humana Medicare Advantage Prescription Drug (MAPD) or commercial plans for patients aged > 18 years with ≥ 1 prescription filled for a DPP-4 inhibitor between July 1, 2011, and March 31, 2013...
March 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28228317/short-term-therapy-with-combination-dipeptidyl-peptidase-4-inhibitor-saxagliptin-metformin-extended-release-xr-is-superior-to-saxagliptin-or-metformin-xr-monotherapy-in-prediabetic-women-with-polycystic-ovary-syndrome-a-single-blind-randomized-pilot-study
#2
Karen E Elkind-Hirsch, Martha S Paterson, Ericka L Seidemann, Hanh C Gutowski
OBJECTIVE: To evaluate efficacy with the dipeptidyl peptidase-4 inhibitor saxagliptin (SAXA), metformin extended release (MET), and combination (SAXA-MET) in patients with polycystic ovary syndrome (PCOS) and impaired glucose regulation. DESIGN: Prospective, randomized, single-blind drug study. SETTING: Outpatient clinic. PATIENT(S): Patients (n = 38) with PCOS (aged 18-42 years) and prediabetic hyperglycemia determined by a 75-gram oral glucose tolerance test...
January 2017: Fertility and Sterility
https://www.readbyqxmd.com/read/28225432/use-of-dipeptidyl-peptidase-4-inhibitors-in-patients-with-type-2-diabetes-and-chronic-kidney-disease
#3
Polly A Bittle
There is a need for treatment options in patients with type 2 diabetes mellitus and kidney disease to achieve glucose targets without risk of hypoglycemia. This article describes management options for these patients using glucose-lowering therapies, in particular dipeptidyl peptidase-4 inhibitors.
February 20, 2017: Nurse Practitioner
https://www.readbyqxmd.com/read/28222401/combination-of-sitagliptin-and-silymarin-ameliorates-liver-fibrosis-induced-by-carbon-tetrachloride-in-rats
#4
Samia Salem Sokar, Magda El-Sayed El-Sayad, Mai El-Sayed Ghoneim, Abdelhadi Mohamed Shebl
Liver fibrosis is a common pathological condition that occurs in most conditions associated with chronic liver injury. Silymarin is a herbal product widely used for its hepatoprotective effect. Sitagliptin, a dipeptidyl peptidase-4 inhibitor (DPP4-I), is clinically used as an oral antidiabetic agent. This study was designed to investigate the effects of Sitagliptin, Silymarin, and their combination on established liver fibrosis in carbon tetrachloride (CCl4) rat model. Male albino rats received intraperitoneal injections of CCl4 three times a week for 7 weeks, as well as daily oral treatments of Sitagliptin (100mg/kg) or Silymarin (100mg/kg) or their combination during the 7 weeks of intoxication...
February 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28222203/defense-related-proteins-involved-in-sugarcane-responses-to-biotic-stress
#5
Thais P Souza, Renata O Dias, Marcio C Silva-Filho
Sugarcane is one of the most important agricultural crops in the world. However, pathogen infection and herbivore attack cause constant losses in yield. Plants respond to pathogen infection by inducing the expression of several protein types, such as glucanases, chitinases, thaumatins, peptidase inhibitors, defensins, catalases and glycoproteins. Proteins induced by pathogenesis are directly or indirectly involved in plant defense, leading to pathogen death or inducing other plant defense responses. Several of these proteins are induced in sugarcane by different pathogens or insects and have antifungal or insecticidal activity...
February 20, 2017: Genetics and Molecular Biology
https://www.readbyqxmd.com/read/28216506/-role-of-dipeptidyl-peptidase-4-and-its-inhibitor-in-the-respiratory-diseases
#6
Yabing Sun, Libing Ma
Dipeptidyl peptidase-4 (DPP-4) is known as a highly conserved type II transmembraneous glycoprotein widely distributed in a variety of tissues and cells, and expressed in the peripheral blood as a soluble form. It has been reported that DPP4 play a distinct role in the physiological and pathological processes, such as immune regulation, inflammatory reaction, cell adhesion, and cell apoptosis. DPP4 inhibitor showes an incredible effect on the control of blood glucose and it is thought as a newly-developed drug for diabetes, especially in regulation of post-prandial glycemia...
January 28, 2017: Zhong Nan da Xue Xue Bao. Yi Xue Ban, Journal of Central South University. Medical Sciences
https://www.readbyqxmd.com/read/28215601/design-and-synthesis-of-quinazoline-3-4-4h-diamine-endowed-with-thiazoline-moiety-as-new-class-for-dpp-4-and-dpph-inhibitor
#7
Zulphikar Ali, Md Jawaid Akhtar, Md Rafi Haider, Ahsan Ahmed Khan, Anees Ahmad Siddiqui, M Shahar Yar
New N3-benzylidene (substituted)-2-phenyl-N4-(thiazol-2-yl)-quinazoline-3,4-(4H)-diamine derivatives were design and synthesized by a sequence of reactions starting from appropriate 6-methyl anthranilic acid. The title compounds were screened for in vitro dipeptidyl peptidase IV (DPP-4) inhibitory activity and diphenyl-2-picryl-hydrazyl (DPPH) assay and results showed significant to good activity in compared to Linagliptin for antidiabetic activity and Ascorbic acid for antioxidant activity. Compound 7g (IC50=0...
February 10, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28215351/a-genomic-comparison-of-putative-pathogenicity-related-gene-families-in-five-members-of-the-ophiostomatales-with-different-lifestyles
#8
Ljerka Lah, Ulrike Löber, Tom Hsiang, Stefanie Hartmann
Ophiostomatoid fungi are vectored by their bark-beetle associates and colonize different host tree species. To survive and proliferate in the host, they have evolved mechanisms for detoxification and elimination of host defence compounds, efficient nutrient sequestration, and, in pathogenic species, virulence towards plants. Here, we assembled a draft genome of the spruce pathogen Ophiostoma bicolor. For our comparative and phylogenetic analyses, we mined the genomes of closely related species (Ophiostoma piceae, Ophiostoma ulmi, Ophiostoma novo-ulmi, and Grosmannia clavigera)...
March 2017: Fungal Biology
https://www.readbyqxmd.com/read/28213955/the-skin-barrier-function-gene-spink5-is-associated-with-challenge-proven-ige-mediated-food-allergy-in-infants
#9
Sarah E Ashley, Hern-Tze Tina Tan, Peter Vuillermin, Shyamali C Dharmage, Mimi L K Tang, Jennifer Koplin, Lyle C Gurrin, Adrian Lowe, Caroline Lodge, Anne-Louise Ponsonby, John Molloy, Pamela Martin, Melanie C Matheson, Richard Saffery, Katrina J Allen, Justine A Ellis, David Martino
BACKGROUND: A defective skin barrier is hypothesised to be an important route of sensitisation to dietary antigens, and may lead to food allergy in some children. Missense mutations in the Serine peptidase inhibitor kazal type 5 (SPINK5) skin barrier gene have previously been associated with allergic conditions. OBJECTIVE: To determine whether genetic variants in and around SPINK5 are associated with IgE mediated food allergy. METHOD: We genotyped 71 'tag' single nucleotide polymorphisms (tag-SNPs) within a region spanning ~263 kilobases (kb) including SPINK5 (~61kb) in n=722 (n=367 food allergic, n=199 food sensitised, tolerant and n=156 non-food allergic controls) 12-month infants (discovery sample) phenotyped for food allergy with the gold standard oral food challenge (OFC)...
February 18, 2017: Allergy
https://www.readbyqxmd.com/read/28211604/delays-in-treatment-intensification-with-oral-antidiabetic-drugs-and-risk-of-microvascular-and-macrovascular-events-in-patients-with-poor-glycemic-control-an-individual-patient-simulation-study
#10
Henry J Folse, Jayanti Mukherjee, John J Sheehan, Alexandra J Ward, Ryan L Pelkey, Tuan A Dinh, Lei Qin, Jennifer Kim
AIMS: Despite guideline recommendations, many patients with type 2 diabetes on oral antidiabetic drugs (OADs) whose HbA1c results remain above target do not experience timely treatment intensification. This study uses the Archimedes Model® to estimate the consequences of delays in OAD treatment intensification on glycemic control and long-term outcomes at 5 and 20 years. MATERIALS AND METHODS: Using real world data, we modeled a cohort of hypothetical patients with HbA1c ≥8%, on metformin, with no history of insulin use...
February 17, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28205322/efficacy-and-safety-of-autoinjected-exenatide-once-weekly-suspension-versus-sitagliptin-or-placebo-with-metformin-in-patients-with-type-2-diabetes-the-duration-neo-2-randomized-clinical-study
#11
Kishore M Gadde, Marion L Vetter, Nayyar Iqbal, Elise Hardy, Peter Öhman
AIMS: Glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors treat type 2 diabetes through incretin-signaling pathways. This study compared the efficacy and safety of the glucagon-like peptide-1 receptor agonist exenatide once-weekly (Miglyol) suspension for autoinjection (QWS-AI) with the dipeptidyl peptidase-4 inhibitor sitagliptin or placebo. MATERIALS AND METHODS: In this open-label, multicenter study of patients with type 2 diabetes who had suboptimal glycemic control on metformin monotherapy, 365 patients were randomized to receive exenatide 2...
February 16, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28201967/dipeptidyl-peptidase-4-inhibitor-induced-angioedema-an-overlooked-and-potentially-lethal-adverse-drug-reaction
#12
Susanne Irene Scott, Michelle Fog Andersen, Lise Aagaard, Christian Von Buchwald, Eva Rye Rasmussen
Introduction Angioedema is a potentially fatal adverse drug reaction of some medications, as swellings of the upper airways can cause death by asphyxiation. Angiotensin converting enzyme-inhibitors are widely known to cause angioedema but less is known about the association between dipeptidyl peptidase-4 inhibitors (gliptins) and angioedema. Dipeptidyl peptidase-4 inhibitors are anti-diabetic drugs used to improve glycaemic control. They, as a class effect, inadvertently affect the degradation of the vasoactive kinins bradykinin and substance P, both of which can cause angioedema due to vasodilatation and increase in vascular permeability in the capillaries...
February 14, 2017: Current Diabetes Reviews
https://www.readbyqxmd.com/read/28197977/interpreting-cardiovascular-endpoints-in-trials-of-antihyperglycemic-drugs
#13
REVIEW
Himika Chawla, Nikhil Tandon
In view of the significant cardiovascular (CV) morbidity and mortality in patients with type 2 diabetes mellitus, and concerns raised about the CV safety of some glucose-lowering drugs, the US Food and Drug Administration (FDA) issued guidance for the industry in 2008 to demonstrate CV safety for the approval of all new antihyperglycemic drugs. Seven randomized controlled trials involving around 60,000 participants have been completed so far and have demonstrated the CV safety of dipeptidyl peptidase 4 inhibitors (saxagliptin, alogliptin and sitagliptin), glucagon-like peptide-1 receptor agonists (lixisenatide, liraglutide and semaglutide) and a sodium-glucose co-transporter 2 inhibitor (empagliflozin) in patients with type 2 diabetes...
February 14, 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/28195389/no-increased-risk-of-cardiovascular-events-in-older-adults-initiating-dipeptidyl-peptidase-4-inhibitors-versus-therapeutic-alternatives
#14
Mugdha Gokhale, John B Buse, Michele Jonsson Funk, Jennifer Lund, Virginia Pate, Ross J Simpson, Til Stürmer
OBJECTIVE: Randomized placebo-controlled trials have examined the cardiovascular (CV) effects of dipeptidyl peptidase-4 inhibitors (DPP-4i), but data on incidence relative to therapeutic alternatives are limited in the older US Medicare population. We compared the CV risk with DPP-4i relative to sulfonylureas (SU) and thiazolidinediones (TZD). METHODS: During 2007-2013, using Medicare beneficiaries >65 years we identified two new-user cohorts without the use of drugs being compared in the 6 months before initiation: DPP-4i versus SU and DPP-4i versus TZD...
February 14, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28194113/cardiovascular-benefits-of-native-glp-1-and-its-metabolites-an-indicator-for-glp-1-therapy-strategies
#15
REVIEW
Junfeng Li, Juan Zheng, Susanne Wang, Harry K Lau, Ali Fathi, Qinghua Wang
Cardiovascular disease is a common co-morbidity and leading cause of death in patients with type 2 diabetes mellitus (T2DM). Glucagon-like peptide 1 (GLP-1) is a peptide hormone produced by intestinal L cells in response to feeding. Native GLP-1 (7-36) amide is rapidly degraded by diaminopeptidyl peptidase-4 (DPP4) to GLP-1 (9-36) amide, making 9-36a the major circulating form. While it is 7-36a, and not its metabolites, which exerts trophic effects on islet β-cells, recent studies suggest that both 7-36a and its metabolites have direct cardiovascular effects, including preserving cardiomyocyte viability, ameliorating cardiac function, and vasodilation...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28192542/functional-diversity-of-secreted-cestode-kunitz-proteins-inhibition-of-serine-peptidases-and-blockade-of-cation-channels
#16
Martín Fló, Mariana Margenat, Leonardo Pellizza, Martín Graña, Rosario Durán, Adriana Báez, Emilio Salceda, Enrique Soto, Beatriz Alvarez, Cecilia Fernández
We previously reported a multigene family of monodomain Kunitz proteins from Echinococcus granulosus (EgKU-1-EgKU-8), and provided evidence that some EgKUs are secreted by larval worms to the host interface. In addition, functional studies and homology modeling suggested that, similar to monodomain Kunitz families present in animal venoms, the E. granulosus family could include peptidase inhibitors as well as channel blockers. Using enzyme kinetics and whole-cell patch-clamp, we now demonstrate that the EgKUs are indeed functionally diverse...
February 13, 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28187861/corrigendum-to-demographic-and-clinical-characteristics-of-type-2-diabetes-mellitus-patients-initiating-dipeptidyl-peptidase-4-inhibitors-a-retrospective-study-of-uk-general-practice-clin-ther-2016-8-1825-1832-e15
#17
Abigail Tebboth, Sally Lee, Anna Scowcroft, Paula Bingham-Gardiner, William Spencer, John Bolodeoku, Syed Wasi Hassan
No abstract text is available yet for this article.
February 7, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28183314/dpp-4-inhibition-has-no-acute-effect-on-bnp-and-its-n-terminal-pro-hormone-measured-by-commercial-immune-assays-a-randomized-cross-over-trial-in-patients-with-type-2-diabetes
#18
Gian Paolo Fadini, Benedetta Maria Bonora, Mattia Albiero, Martina Zaninotto, Mario Plebani, Angelo Avogaro
BACKGROUND: Use of dipeptidyl peptidase-4 inhibitors (DPP4-i) for the treatment of type 2 diabetes (T2D) has been associated with a possible increase in the risk for heart failure (HF). B-type natriuretic peptide (BNP), which is both a biomarker of HF and a hemodynamically active hormone, is a substrate of DPP-4. We herein tested the acute effects of the DPP-4i linagliptin on BNP and NT-proBNP in a cross-over placebo-controlled trial in patients with T2D with and without chronic kidney disease (CKD)...
February 10, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28183185/rational-design-of-selective-and-bioactive-inhibitors-of-the-mycobacterium-tuberculosis-proteasome
#19
Kyle A Totaro, Dominik Barthelme, Peter T Simpson, Xiuju Jiang, Gang Lin, Carl F Nathan, Robert T Sauer, Jason K Sello
The 20S core particle of the proteasome in Mycobacterium tuberculosis (Mtb) is a promising, yet unconventional, drug target. This multimeric peptidase is not essential, yet degrades proteins that have become damaged and toxic via reactions with nitric oxide (and/or the associated reactive nitrogen intermediates) produced during the host immune response. Proteasome inhibitors could render Mtb susceptible to the immune system, but they would only be therapeutically viable if they do not inhibit the essential 20S counterpart in humans...
February 10, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28182722/hemoglobin-glycation-index-as-a-useful-predictor-of-therapeutic-responses-to-dipeptidyl-peptidase-4-inhibitors-in-patients-with-type-2-diabetes
#20
Yu-Wei Chen, Jun-Sing Wang, Wayne H-H Sheu, Shih-Yi Lin, I-Te Lee, Yuh-Min Song, Chia-Po Fu, Chia-Lin Lee
INTRODUCTION: A high hemoglobin glycation index (HGI) and glycated hemoglobin (HbA1c) level are associated with greater inflammatory status, and dipeptidyl peptidase-4 (DPP-4) inhibitors can suppress inflammation. We aimed to evaluate the relationship between HGI and the therapeutic effect of DPP-4 inhibitors. METHODS: This retrospective cohort study followed 468 patients with type 2 diabetes receiving DPP-4 inhibitor treatment for 1 year. Estimated HbA1c was calculated using a linear regression equation derived from another 2969 randomly extracted patients with type 2 diabetes based on fasting plasma glucose (FPG) level...
2017: PloS One
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