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https://www.readbyqxmd.com/read/28411801/optimization-of-gold-nanoparticle-based-real-time-colorimetric-assay-of-dipeptidyl-peptidase-iv-activity
#1
Hasan Saad Aldewachi, Nicola Woodroofe, Simon Turega, Philip H E Gardiner
Dipeptidyl peptidase IV (DPP-IV also referred to as CD-26) is a serine protease enzyme with remarkable diagnostic and prognostic value in a variety of health and disease conditions. Herein, we describe a simple and real-time colorimetric assay for DPP-IV/CD-26 activity based on the aggregation of gold nanoparticles (AuNPs) functionalized with the peptide substrates: Gly-Pro-Asp-Cys (GPDC) or Val-Pro-ethylene diamine-Asp-Cys (VP-ED-DC). Cleavage of the substrates by DPP-IV resulted in aggregation of the AuNPs with accompanying color change in the solution from red to blue that was monitored using either a UV-visible spectrophotometer or by the naked eye...
July 1, 2017: Talanta
https://www.readbyqxmd.com/read/28406239/cmd-05-a-novel-promising-clinical-anti-diabetic-drug-candidate-in-vivo-and-vitro-studies
#2
Jie Ma, Huan Li, Xiangnan Hu, Lu Yang, Qi Chen, Congli Hu, Zhihao Chen, Xiaoyan Tian, Yang Yang, Ying Luo, Run Gan, Junqing Yang
Dipeptidyl peptidase IV (DPP-IV) inhibitor has been expected to be a new class of anti-diabetic agent. The present study was designed to characterize the pharmacological profiles of CMD-05, a novel DPP-IV inhibitor discovered in our laboratory, in vitro and in vivo. The IC50 of CMD-05 on DPP-IV inhibitory activity was approximately 12 nM while vildagliptin was 3.5 nM in vitro. In diabetes rat model established by high fat diet/low dose streptozotocin, CMD-05 inhibited DPP-IV activity, significantly improved glucose tolerance, increased GLP-1 and insulin levels in plasma...
April 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28402172/rational-design-and-synthesis-of-affinity-matrices-based-on-proteases-immobilized-onto-cellulose-membranes
#3
Alberto Del Monte-Martínez, Jorge González-Bacerio, Bessy Cutiño-Avila, Jorge Rojas, Mae Chappé, Emir Salas-Sarduy, Isel Pascual, José M Guisán
Discovery of new protease inhibitors may result in potential therapeutic agents or useful biotechnological tools. Obtainment of these molecules from natural sources requires simple, economic and highly efficient purification protocols. The aim of this work was the obtainment of affinity matrices by the covalent immobilization of dipeptidyl peptidase IV (DPP-IV) and papain onto cellulose membranes, previously activated with formyl (FCM) or glyoxyl groups (GCM). GCM showed the highest activation grade (10.2 µmol aldehyde/cm(2))...
April 12, 2017: Preparative Biochemistry & Biotechnology
https://www.readbyqxmd.com/read/28376103/correction-of-vitamin-d-deficiency-facilitated-suppression-of-ip-10-and-dpp-iv-levels-in-patients-with-chronic-hepatitis-c-a-randomised-double-blinded-placebo-control-trial
#4
Piyawat Komolmit, Kriangsak Charoensuk, Kessarin Thanapirom, Sirinporn Suksawatamnuay, Panarat Thaimai, Chintana Chirathaworn, Yong Poovorawan
Vitamin D deficiency was common among patients with chronic hepatitis C (CHC) and had negative influence on treatment outcome. Correction of vitamin D deficiency improved treatment response. Interferon gamma-induced protein 10 (IP-10) and enzyme dipeptidyl peptidase-4 (DPP IV) involved in inflammatory responses in CHC. Their higher levels at pretreatment of CHC could predict poorer responses. Vitamin D suppressed expression of IP-10 from monocytes in vitro. In CHC patients, DPP IV involved in IP-10 regulation...
2017: PloS One
https://www.readbyqxmd.com/read/28351157/synthetic-and-phytocompounds-based-dipeptidyl-peptidase-iv-dpp-iv-inhibitors-for-therapeutics-of-diabetes
#5
Anand-Krishna Singh, Rameshwar Jatwa, Ashok Purohit, Heera Ram
Currently antidiabetic therapeutic strategies are mainly based on synthetic hypoglycemic agent. Antidiabetic drugs are associated with significant adverse effects of hypoglycemia, dysfunction of insulin and weight gain. Nowadays, the novel Dipeptidyl peptidase-IV (DPP-IV) inhibitors unique approach for the management of diabetes has been considered to be safe, as DPP-IV inhibitors reduce blood glucose level by monitoring hyperglycemia including positive effects on body weight as it remains neutral, improves glycated hemoglobin levels and do not induce hypoglycemia...
March 29, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28344207/dipeptidyl-peptidase-iv-inhibition-for-the-treatment-of-cardiovascular-disease%C3%A3-recent-insights-focusing-on-angiogenesis-and-neovascularization
#6
Yanna Lei, Lina Hu, Guang Yang, Limei Piao, Minggen Jin, Xianwu Cheng
Dipeptidyl peptidase IV (DPP-IV) is a complex enzyme that acts as a membrane-anchored cell surface exopeptidase and transmits intracellular signals through a small intracellular tail. DPP-IV exists in human blood in a soluble form, and truncates a large number of peptide hormones, chemokines, cytokines, and growth factors in vitro and in vivo. DPP-IV has gained considerable interest as a therapeutic target, and a variety of DPP-IV inhibitors that prolong the insulinotropic effects of glucagon-like peptide-1 (GLP-1) are widely used in clinical settings as antidiabetic drugs...
March 25, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/28326327/ameliorating-effect-of-gemigliptin-on-renal-injury-in-murine-adriamycin-induced-nephropathy
#7
Da Rae Kim, Shin Yeong Lee, Jin Sug Kim, Yang Gyun Kim, Ju-Young Moon, Sang Ho Lee, Tae Won Lee, Chun Gyoo Ihm, Kyung Hwan Jeong
Background. Previous studies have shown the antiapoptotic and anti-inflammatory potential of DPP-IV inhibitor in experimental models of renal injury. We tested whether DPP-IV inhibitor (gemigliptin) ameliorates renal injury by suppressing apoptosis, inflammation, and oxidative stress in mice with adriamycin nephropathy. Methods. Mice were treated with normal saline (control), gemigliptin (GM), adriamycin (ADR), or adriamycin combined with gemigliptin (ADR+GM). Apoptosis, inflammation, and oxidative stress were analyzed via western blotting, real-time PCR, light microscopy, and immunofluorescence...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28318663/dipeptidyl-peptidase-iv-in-chronic-heart-failure-with-reduced-ejection-fraction
#8
Patrícia Lourenço, Sérgio Silva, Filipe Cunha, Joana Pereira, Ana Ribeiro, Nuno Silva, João Tiago Guimarães, José Paulo Araújo, Paulo Bettencourt
BACKGROUND: An association between dipeptidyl peptidase-IV (DPP-IV) inhibitors with worse prognosis in HF has been suggested. We aimed to assess the serum DPP-IV levels in chronic stable HF patients and determine their association with prognosis. METHODS AND RESULTS: Chronic stable HF patients with optimized prognostic-modifying therapy were prospectively recruited. EXCLUSION CRITERIA: 1) ejection fraction>50%, 2) hospitalizations or therapeutic adjustments in the previous 2months; 3) patients on renal replacement therapy, and 4) use of DPP-IV inhibitors...
March 11, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28292762/gpr40-reduces-food-intake-and-body-weight-through-glp-1
#9
Judith N Gorski, Michele J Pachanski, Joel Mane, Christopher W Plummer, Sarah Souza, Brande S Thomas-Fowlkes, Aimie M Ogawa, Adam B Weinglass, Jerry Di Salvo, Boonlert Cheewatrakoolpong, Andrew D Howard, Steven L Colletti, Maria E Trujillo
GPR40 partial agonists lower glucose through the potentiation of glucose-stimulated insulin secretion, which is believed to provide significant glucose lowering without the weight gain or hypoglycemic risk associated with exogenous insulin or glucose independent insulin secretagogues. The class of small molecule GPR40 modulators, known as AgoPAMs (agonist also capable of acting as positive allosteric modulators), differentiate from partial agonists, binding to a distinct site and functioning as full agonists to stimulate the secretion of both insulin and GLP-1 (17)...
March 14, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28290371/release-of-dipeptidyl-peptidase-iv-dpp-iv-inhibitory-peptides-from-milk-protein-isolate-mpi-during-enzymatic-hydrolysis
#10
Alice B Nongonierma, Caterina Mazzocchi, Sara Paolella, Richard J FitzGerald
The release of dipeptidyl peptidase IV (DPP-IV) inhibitory peptides from bovine milk protein isolate (MPI) during trypsin hydrolysis was studied using a design of experiments (DOE) approach. A 3 factor×3 level DOE including temperature (40, 50 and 60°C), enzyme to substrate ratio (E:S; 0.50, 1.25 and 2.00% (w/w)) and hydrolysis time (60, 150 and 240min) was used during the generation of 15 hydrolysates (H1-H15). The degree of hydrolysis (DH) varied between 6.98±0.31 (H8) to 12.75±0.62% (H10). The DPP-IV half maximal inhibitory concentration (IC50) ranged from 0...
April 2017: Food Research International
https://www.readbyqxmd.com/read/28290288/using-caco-2-cells-as-novel-identification-tool-for-food-derived-dpp-iv-inhibitors
#11
Juliette Caron, Dorothée Domenger, Pascal Dhulster, Rozenn Ravallec, Benoit Cudennec
Dietary proteins have recently been investigated as a new source of DPP-IV inhibitory peptides with limited side effects and promising applications. Numerous studies have highlighted and identified peptide sequences able to inhibit DPP-IV activity in vitro, mostly from milk proteins. However, the correlation to in vivo studies remains scarce because standard in vitro assays with purified enzyme do not accurately simulate key factors impacting peptide bioactivity such as intestinal and brush border enzymes or cellular permeability...
February 2017: Food Research International
https://www.readbyqxmd.com/read/28276830/bariatric-surgery-time-to-replace-with-glp-1
#12
Dominic-Luc Webb, Niclas Abrahamsson, Magnus Sundbom, Per M Hellström
Obesity with a body mass index (BMI) over 30 kg/m(2) represents a significant risk for increased morbidity and mortality, with reduced life expectancy of about 10 years. Until now, surgical treatment has been the only effective longterm intervention. The currently standardized method of bariatric surgery, gastric bypass, means that many gastrointestinal peptide hormones are activated, yielding net reductions in appetite and food intake. Among the most important gut peptide hormones in this perspective is glucagon-like peptide-1 (GLP-1), which rises sharply after gastric bypass...
June 2017: Scandinavian Journal of Gastroenterology
https://www.readbyqxmd.com/read/28155144/enzyme-histochemistry-technique-for-visualizing-the-dipeptidyl-peptidase-iv-dpp-iv-activity-in-the-liver-biliary-tree
#13
Vittorio Bertone, Eleonora Tarantola, Isabel Freitas
Dipeptidyl-peptidase IV is an enzyme involved in a lot of biochemical processes, where it modifies a number of regulatory proteins by removing the terminal peptides by hydrolysis. Here we describe a histochemical method to demonstrate with accuracy and precision its in situ activity on cryostatic section of Wistar rat liver by means of a simultaneous azo-coupling method.
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28155089/predicting-dpp-iv-inhibitors-with-machine-learning-approaches
#14
Jie Cai, Chanjuan Li, Zhihong Liu, Jiewen Du, Jiming Ye, Qiong Gu, Jun Xu
Dipeptidyl peptidase IV (DPP-IV) is a promising Type 2 diabetes mellitus (T2DM) drug target. DPP-IV inhibitors prolong the action of glucagon-like peptide-1 (GLP-1) and gastric inhibitory peptide (GIP), improve glucose homeostasis without weight gain, edema, and hypoglycemia. However, the marketed DPP-IV inhibitors have adverse effects such as nasopharyngitis, headache, nausea, hypersensitivity, skin reactions and pancreatitis. Therefore, it is still expected for novel DPP-IV inhibitors with minimal adverse effects...
February 2, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28119159/hindbrain-dpp-iv-inhibition-improves-glycemic-control-and-promotes-negative-energy-balance
#15
Elizabeth G Mietlicki-Baase, Lauren E McGrath, Kieran Koch-Laskowski, Joanna Krawczyk, Tram Pham, Rinzin Lhamo, David J Reiner, Matthew R Hayes
The beneficial glycemic and food intake-suppressive effects of glucagon-like peptide-1 (GLP-1) have made this neuroendocrine system a leading target for pharmacological approaches to the treatment of diabetes and obesity. One strategy to increase the activity of endogenous GLP-1 is to prevent the rapid degradation of the hormone by the enzyme dipeptidyl peptidase-IV (DPP-IV). However, despite the expression of both DPP-IV and GLP-1 in the brain, and the clear importance of central GLP-1 receptor (GLP-1R) signaling for glycemic and energy balance control, the metabolic effects of central inhibition of DPP-IV activity are unclear...
May 1, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28098291/investigation-into-the-bioavailability-of-milk-protein-derived-peptides-with-dipeptidyl-peptidase-iv-inhibitory-activity-using-caco-2-cell-monolayers
#16
Isabelle M E Lacroix, Xiu-Min Chen, David D Kitts, Eunice C Y Li-Chan
In recent years, peptides derived from a variety of dietary proteins have been reported to exhibit inhibitory activity against the dipeptidyl-peptidase IV (DPP-IV) enzyme, a target in the management of type 2 diabetes. While much attention has been given to the production and identification of peptides with DPP-IV inhibitory activity from food proteins, particularly dairy proteins, little is known on the bioavailability of these molecules. In this study, the stability and transport of five previously identified milk-derived peptides (LKPTPEGDL, LPYPY, IPIQY, IPI and WR) and a whey protein isolate (WPI) digest with DPP-IV-inhibitory activity were investigated using Caco-2 cell monolayers as a model system for human intestinal absorption...
February 22, 2017: Food & Function
https://www.readbyqxmd.com/read/28062644/ligand-induced-conformational-changes-in-prolyl-oligopeptidase-a-kinetic-approach
#17
R Van Elzen, E Schoenmakers, I Brandt, P Van Der Veken, A M Lambeir
Most kinetic studies of prolyl oligopeptidase (PREP) were performed with the porcine enzyme using modified peptide substrates. Yet recent biophysical studies used the human homolog. Therefore, the aim of this study was to compare the kinetic behavior of human and porcine PREP, as well as to find a suitable method to study enzyme kinetics with an unmodified biological substrate. It was found that human PREP behaves identically to the porcine homolog, displaying a double bell-shaped pH profile and a pH-dependent solvent kinetic isotope effect of the kcat/Km, features that set it apart from the related exopeptidase dipeptidyl peptidase IV (DPP IV)...
March 1, 2017: Protein Engineering, Design & Selection: PEDS
https://www.readbyqxmd.com/read/27990119/oral-administration-of-sitagliptin-activates-creb-and-is-neuroprotective-in-murine-model-of-brain-trauma
#18
Brian DellaValle, Gitte S Brix, Birgitte Brock, Michael Gejl, Jørgen Rungby, Agnete Larsen
Introduction: Traumatic brain injury is a major cause of mortality and morbidity. We have previously shown that the injectable glucagon-like peptide-1 (GLP-1) analog, liraglutide, significantly improved the outcome in mice after severe traumatic brain injury (TBI). In this study we are interested in the effects of oral treatment of a different class of GLP-1 based therapy, dipeptidyl peptidase IV (DPP-IV) inhibition on mice after TBI. DPP-IV inhibitors reduce the degradation of endogenous GLP-1 and extend circulation of this protective peptide in the bloodstream...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27983830/peptides-derived-from-soy-and-lupin-protein-as-dipeptidyl-peptidase-iv-inhibitors-in-vitro-biochemical-screening-and-in-silico-molecular-modeling-study
#19
Carmen Lammi, Chiara Zanoni, Anna Arnoldi, Giulio Vistoli
Dipeptidyl peptidase IV (DPP-IV) is a new molecular target correlated with the development of type 2 diabetes. Literature describes the identification of some inhibitory peptides from the hydrolysis of different food proteins. This article reports a study on six peptides from soybean and lupin proteins, i.e., Soy 1 (IAVPTGVA), Soy 2 (YVVNPDNDEN), Soy 3 (YVVNPDNNEN), Lup 1 (LTFPGSAED), Lup 2 (LILPKHSDAD), and Lup 3 (GQEQSHQDEGVIVR), which were screened for their capacity to inhibit the activity of DPP-IV, using an in vitro bioassay against human recombinant DPP-IV...
December 28, 2016: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/27970351/tct-180-impact-of-the-novel-dpp-iv-inhibitor-dutogliptin-in-combination-with%C3%A2-g-csf-on-survival-rates-and-cardiac-remodelling-after-acute-myocardial%C3%A2-infarction
#20
Roman Schenk, Darrell Nix
No abstract text is available yet for this article.
November 1, 2016: Journal of the American College of Cardiology
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