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https://www.readbyqxmd.com/read/28619366/bpi-3016-a-novel-long-acting-hglp-1-analogue-for-the-treatment-of-type-2-diabetes-mellitus
#1
Lieming Ding, Sisi Lu, Yanping Wang, Haibo Chen, Wei Long, Cunbo Ma, Erlong He, Dan Yan, Fenlai Tan
Glucagon-like peptide-1 (GLP-1) analogues have been commonly used as add-on medications for patients with Type 2 diabetes mellitus (T2DM). Currently, the development of long-acting GLP-1 analogues which allow the freedom and flexibility of once-weekly injections while maintaining their potency for a relatively long period has become the mainstream. Here, we successfully developed a long-acting human GLP-1(7-37) analogue (BPI-3016) with significantly extended half-life and increased resistance to dipeptidyl peptidase IV (DPP-IV) cleavage by structural modifications of human GLP-1...
June 13, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28599787/anti-cd26-autoantibodies-are-involved-in-rheumatoid-arthritis-and-show-potential-clinical-interest
#2
Oscar J Cordero, Rubén Varela-Calviño, Tania López-González, Milica Grujic, Zorica Juranic, Coral Mouriño, Íñigo Hernández-Rodríguez, Marina Rodríguez-López, Bruno Aspe de la Iglesia, José María Pego-Reigosa
OBJECTIVES: Rheumatoid arthritis (RA) patients show low serum levels of the Ag dipeptidyl peptidase IV (DPP-IV/CD26), both soluble CD26 (sCD26) concentration and its DPP-IV activity. The aim of this study was to test if anti-DPP-IV/CD26 Abs (Anti-CD26) cleared sCD26. DESIGN & METHODS: Serum Anti-CD26 and Total titers (as comparison) of isotypes IgA, IgM and IgG as well as sCD26 concentration and DPP-IV activity were measured in a cohort of RA patients undergoing different biological and non-biological therapies (n=105) and controls (n=50)...
June 6, 2017: Clinical Biochemistry
https://www.readbyqxmd.com/read/28593550/yh18421-a-novel-gpr119-agonist-exerts-sustained-glucose-lowering-and-weight-loss-in-diabetic-mouse-model
#3
Yoo Hoi Park, Hyun Ho Choi, Dong Hoon Lee, Soo Yong Chung, Na Yeon Yang, Do Hoon Kim, Mi Kyeong Ju, Tae Dong Han, Su Youn Nam, Kyu-Won Kim
G-protein-coupled receptor 119 (GPR119) represents a promising target for the treatment of type 2 diabetes as it can increase both GLP-1 secretion from intestinal L cells and glucose-stimulated insulin secretion (GSIS) from pancreatic β cells. Due to this dual mechanism of action, the development of small molecule GPR119 agonists has received much interest for the treatment of type 2 diabetes. Here, we identified a novel small-molecule GPR119 agonist, YH18421 and evaluated its therapeutic potential. YH18421 specifically activated human GPR119 with high potency and potentiated GLP-1 secretion and GSIS in vitro cell based systems...
June 8, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28556182/two-novel-bioactive-peptides-from-antarctic-krill-with-dual-angiotensin-converting-enzyme-and-dipeptidyl-peptidase-iv-inhibitory-activities
#4
Wei Ji, Chaohua Zhang, Hongwu Ji
Inhibition of dipeptidyl peptidase IV (DPP-IV) and angiotensin converting enzyme (ACE) are considered useful in managing 2 often associated conditions: diabetes and hypertension. In this study, corolase PP was used to hydrolyze Antarctic krill protein. The hydrolysate (AKH) was isolated by ultrafiltration and purified by size-exclusion chromatography, ion exchange chromatography and reversed-phase high-performance liquid chromatography (RP-HPLC) sequentially. The in vitro inhibitory activities of all AKHs and several fractions obtained against ACE and DPP-IV were assessed...
May 27, 2017: Journal of Food Science
https://www.readbyqxmd.com/read/28551257/a-study-to-evaluate-the-potential-of-an-in-silico-approach-for-predicting-dipeptidyl-peptidase-iv-inhibitory-activity-in-vitro-of-protein-hydrolysates
#5
Tzu-Yuan Wang, Cheng-Hong Hsieh, Chuan-Chuan Hung, Chia-Ling Jao, Pei-Yi Lin, You-Liang Hsieh, Kuo-Chiang Hsu
A total of 294 edible protein sequences and 5 commercial proteases listed in the BIOPEP database were analyzed in silico. The frequency (A), a parameter in silico described previously, was examined further to calculating the ratio of truncated peptides with Xaa-proline and/or Xaa-alanine to all peptide fragments in a protein hydrolyzed with a protease, using the BIOPEP database. Then the in vitro DPP-IV inhibitory activity was determined using the same 15 protein and protease combinations to evaluate their relationship...
November 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28534590/generation-of-wheat-gluten-hydrolysates-with-dipeptidyl-peptidase-iv-dpp-iv-inhibitory-properties
#6
A B Nongonierma, M Hennemann, S Paolella, R J FitzGerald
Wheat gluten, a Pro-rich dietary protein, was investigated for its potential to produce dipeptidyl peptidase IV (DPP-IV) inhibitory peptides during enzymatic hydrolysis with Debitrase HYW20. Nine gluten hydrolysates (H1-H9) were generated using a 2 factor × 3 level design of experiments (DOE) including the incubation temperature (40, 50 and 60 °C) and the enzyme: substrate ratio (E : S, 0.5, 1.0 and 1.5% (w/w)). Their DPP-IV half maximal inhibitory concentration (IC50) ranged from 0.24 ± 0.02 (H9) to 0...
May 23, 2017: Food & Function
https://www.readbyqxmd.com/read/28528097/protein-digestomic-analysis-reveals-the-bioactivity-of-deer-antler-velvet-in-simulated-gastrointestinal-digestion
#7
Yang Yu, Yan Jin, Fangjun Wang, Jiaze Yan, Yanxia Qi, Mingliang Ye
Proteins are the most prominent bioactive component in deer antler velvet. The aim of the present study was to track the fate of protein of antler velvet by protein digestomics. The peptide profile identified by LC-MS/MS and the in vitro bioactivity of antler velvet aqueous extract (AAE) were investigated in simulated gastrointestinal digestion. A total of 23, 387 and 417 peptides in AAE, gastric and pancreatic digests were identified using LC-MS/MS, respectively. Collagens, the predominant proteins, released 34 peptides in gastric digests and 146 peptides in pancreatic digests...
June 2017: Food Research International
https://www.readbyqxmd.com/read/28522195/a-dpp-iv-resistant-glucagon-like-peptide-2-dimer-with-enhanced-activity-against-radiation-induced-intestinal-injury
#8
Jintao Gu, Shuo Liu, Nan Mu, Tonglie Huang, Wangqian Zhang, Huadong Zhao, Zhen Shu, Cun Zhang, Qiang Hao, Weina Li, Xiaochang Xue, Wei Zhang, Yingqi Zhang
Although radiotherapy is a highly effective treatment for abdominal or pelvic cancer patients, it can increase the incidence of severe gastrointestinal (GI) toxicity. As an intestinal growth factor, glucagon-like peptide 2 (GLP-2) has been shown to improve the preclinical models of both short bowel syndrome and inflammatory bowel disease by stimulating intestinal growth. Teduglutide ([Gly(2)]GLP-2), a recombinant human GLP-2 variant, has a prolonged half-life and stability as compared to the native GLP-2 peptide, but still requires daily application in the clinic...
May 15, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28512596/in-vitro-screening-for-protein-tyrosine-phosphatase-1b-and-dipeptidyl-peptidase-iv-inhibitors-from-selected-nigerian-medicinal-plants
#9
Yusuf Saidu, Suleiman Alhaji Muhammad, Abdullahi Yahaya Abbas, Andrew Onu, Ibrahim Mohammed Tsado, Luba Muhammad
BACKGROUND/AIM: Protein tyrosine phosphatase 1B (PTP 1B) and dipeptidyl peptidase IV (DPP IV) have been identified as one of the drug targets for the treatment of Type-2 diabetes. This study was designed to screen for PTP 1B and DPP-IV inhibitors from some Nigerian medicinal plants. MATERIALS AND METHODS: PTP 1B and DPP-IV drug discovery kits from Enzo Life Sciences were used to investigate in vitro inhibitory effect of crude methanolic extract of 10 plants; Mangifera indica, Moringa oleifera, Acacia nilotica, Arachis hypogaea, Senna nigricans, Azadirachta indica, Calotropis procera, Leptadenia hastata, Ziziphus mauritiana, and Solanum incanum...
April 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28486736/comparison-of-the-effects-of-mitiglinide-and-glibenclamide-administered-in-combination-with-the-dipeptidyl-peptidase-iv-inhibitor-sitagliptin-in-rats-with-streptozotocin-nicotinamide-induced-type-2-diabetes
#10
Kenji Akahane, Kazuma Ojima, Ayaka Yokoyama, Toshihiro Inoue, Sumiyoshi Kiguchi, Satoshi Tatemichi, Hiroo Takeda, Mamoru Kobayashi
We compared the individual effects of mitiglinide and glibenclamide administered in combination with the dipeptidyl peptidase-IV (DPP-IV) inhibitor sitagliptin on plasma DPP-IV activity and blood glucose levels in rats with streptozotocin-nicotinamide-induced type 2 diabetes (STZ-NA rats). We examined the inhibitory activity of mitiglinide and glibenclamide as well as their combination with sitagliptin on plasma DPP-IV activity in STZ-NA rats. The oral glucose tolerance test (OGTT) was used to compare effects of mitiglinide, glibenclamide, and their combination with sitagliptin on blood glucose levels in STZ-NA rats...
May 9, 2017: Drug Research
https://www.readbyqxmd.com/read/28460928/simulated-gi-digestion-of-dietary-protein-release-of-new-bioactive-peptides-involved-in-gut-hormone-secretion
#11
Juliette Caron, Benoit Cudennec, Dorothée Domenger, Yanath Belguesmia, Christophe Flahaut, Mostafa Kouach, Jean Lesage, Jean-François Goossens, Pascal Dhulster, Rozenn Ravallec
Dietary proteins have been reported to induce a strong feeling of satiety that has been partially explained by gut hormone level increase. Up to date, various protein hydrolysates have demonstrated in vitro and in vivo their potential to stimulate gut hormone secretion related to food intake decrease and their mechanisms of action have just started to be resolved. In this context, this study aimed at identifying new peptide sequences involved in gut hormone secretion released by protein in vitro gastrointestinal digestion...
November 2016: Food Research International
https://www.readbyqxmd.com/read/28452380/heterogeneity-of-molecular-forms-of-dipeptidyl-peptidase-iv-and-fibroblast-activation-protein-in-human-glioblastomas
#12
Ivana Matrasova, Petr Busek, Eva Balaziova, Aleksi Sedo
BACKGROUND AND AIMS: Proteolytic enzymes contribute to the progression of various cancers. We previously reported increased expression of the proline specific peptidases dipeptidyl peptidase-IV (DPP-IV) and its closest paralogue fibroblast activation protein (FAP) in human glioblastomas. Here we analyze the molecular heterogeneity of DPP-IV and FAP in glioblastomas. METHODS: ELISA, isoelectric focusing, 1D and 2D electrophoresis followed by WB or enzyme overlay assay were utilized to analyze DPP-IV and FAP isoforms...
April 26, 2017: Biomedical Papers of the Medical Faculty of the University Palacký, Olomouc, Czechoslovakia
https://www.readbyqxmd.com/read/28449998/milk-protein-isolate-mpi-as-a-source-of-dipeptidyl-peptidase-iv-dpp-iv-inhibitory-peptides
#13
Alice B Nongonierma, Mehdeeyah Lalmahomed, Sara Paolella, Richard J FitzGerald
A multifactorial [temperature (40, 50 and 60°C), hydrolysis time (60, 150 and 240min) and enzyme to substrate ratio (E:S; 1.0, 1.5 and 2.0%)] design of experiments (DOE) was used to optimise the release of dipeptidyl peptidase IV (DPP-IV) inhibitory peptides during hydrolysis of bovine milk protein isolate (MPI) with Neutrase 0.8L™, yielding 15 hydrolysates (H1-H15). Variation in temperature and time had a significant effect on DPP-IV inhibitory properties (p<0.05) in contrast with E:S (p>0.05). The DPP-IV half maximal inhibitory concentration (IC50) of H4, a potent sample, was maintained following simulated gastrointestinal digestion (SGID, DPP-IV IC50=0...
September 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28440199/anti-hyperglycemic-agents-for-the-treatment-of-type-2-diabetes-mellitus-role-in-cardioprotection-during-the-last-decade
#14
Duygu Kocyigit, Kadri Murat Gurses, Muhammed Ulvi Yalcin, Lale Tokgozoglu
Type 2 diabetic patients are known to have a tendency to develop cardiovascular (CV) disease (CVD), and related unfavourable outcomes such as heart failure, myocardial infarction (MI), cerebrovascular events (eg. stroke), and related mortality. Long- term clinical trials have revealed contradictory findings regarding the relationship between glycemic control and CV benefits due to variations in the key characteristics of the study population. During the last decade, number of pharmacological agents used for glucose- lowering in the treatment of type 2 diabetes mellitus (T2DM) has increased owing to the introduction of dipeptidyl peptidase- IV (DPP- IV) inhibitors, glucagon- like peptide- 1 (GLP- 1) receptor agonists, and sodium-glucose co-transporter 2 (SGLT- 2) inhibitors...
April 23, 2017: Endocrine, Metabolic & Immune Disorders Drug Targets
https://www.readbyqxmd.com/read/28433470/daily-supplementation-of-dietary-protein-improves-the-metabolic-effects-of-glp-1-based-pharmacotherapy-in-lean-and-obese-rats
#15
Elizabeth G Mietlicki-Baase, Kieran Koch-Laskowski, Lauren E McGrath, Joanna Krawczyk, Tram Pham, Rinzin Lhamo, David J Reiner, Matthew R Hayes
Glucagon-like peptide-1 (GLP-1) is an incretin hormone released from intestinal L-cells in response to food entering into the gastrointestinal tract. GLP-1-based pharmaceuticals improve blood glucose regulation and reduce feeding. Specific macronutrients, when ingested, may trigger GLP-1 secretion and enhance the effects of systemic sitagliptin, a pharmacological inhibitor of DPP-IV (an enzyme that rapidly degrades GLP-1). In particular, macronutrient constituents found in dairy foods may act as potent secretagogues for GLP-1, and acute preclinical trials show that ingestion of dairy protein may represent a promising adjunct behavioral therapy in combination with sitagliptin...
August 1, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28411801/optimization-of-gold-nanoparticle-based-real-time-colorimetric-assay-of-dipeptidyl-peptidase-iv-activity
#16
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
#17
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
#18
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
#19
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
#20
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
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