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Peptidase inhibitor

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https://www.readbyqxmd.com/read/28323997/degradation-paradigm-of-the-gut-hormone-pancreatic-polypeptide-by-hepatic-and-renal-peptidases
#1
Joyceline Cuenco, James Minnion, Tricia Tan, Rebecca Scott, Natacha Germain, Yiin Ling, Rong Chen, Mohammad Ghatei, Stephen Bloom
Pancreatic polypeptide (PP) is a gut hormone that acts on Y4 receptors to reduce appetite. Obese humans display a reduced postprandial rise in PP and remain fully sensitive to the anorectic effects of exogenous PP. The utility of PP as an antiobesity treatment is limited by its short circulating half-life. Insight into the mechanisms by which PP is degraded may aid design of long-acting PP analogues.We aimed to investigate the role of peptidases in PP degradation with a view to determining whether inhibition of these enzymes enhanced PP plasma levels and bioactivity in vivo...
March 9, 2017: Endocrinology
https://www.readbyqxmd.com/read/28323503/add-on-dpp-4-inhibitor-alogliptin-alone-or-in-combination-with-pioglitazone-improved-%C3%AE-cell-function-and-insulin-sensitivity-in-metformin-treated-pcos
#2
Mojca Jensterle, Katja Goricar, Andrej Janez
PURPOSE: Impaired β-cell function remains unaddressed in PCOS. The aim of the study was to evaluate whether dipeptidyl peptidase-4 (DPP-4) inhibitor alogliptin (ALO) alone or in combination with pioglitazone (PIO) improves β-cell function along with insulin resistance (IR) in metformin (MET) treated obese women with PCOS with persistent IR. MATERIALS AND METHODS: In 12-week randomized study, ALO 25 mg QD (n=15) or ALO 25 mg QD and PIO 30 mg QD (n=15) was added to MET 1000 mg BID in PCOS women (aged 34...
March 21, 2017: Endocrine Research
https://www.readbyqxmd.com/read/28318663/dipeptidyl-peptidase-iv-in-chronic-heart-failure-with-reduced-ejection-fraction
#3
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/28314484/impact-of-health-policy-and-practice-on-finding-the-best-fit-for-patients-with-type-2-diabetes-after-metformin-failure-croatian-pilot-study
#4
Maja Cigrovski Berković, Davorka Herman Mahečić, Marina Gradišer, Ines Bilić-Ćurčić
AIM: We assessed the impact of clinical practice and health policy on the choice and efficacy of different second-line therapies for the treatment of type 2 diabetes (T2DM) after failure of metformin. METHODS: This retrospective database analysis included 200 patients with a follow-up period of 6 months. The primary end-point was achievement of HbA1c <7% and fasting (FBG) and postprandial glucose levels (PPG) <7.2mmol/L and <10mmol/L, respectively after three and six months of different add-on treatments...
March 14, 2017: Primary Care Diabetes
https://www.readbyqxmd.com/read/28302310/design-synthesis-and-anti-diabetic-activity-of-triazolotriazine-derivatives-as-dipeptidyl-peptidase-4-dpp-4-inhibitors
#5
Bhumika D Patel, Shraddha V Bhadada, Manjunath D Ghate
Type 2 diabetes mellitus (T2DM) is one of the major global metabolic disorders characterized by insulin resistance and chronic hyperglycemia. Inhibition of the enzyme, dipeptidyl peptidase-4 (DPP-4) has been proved as successful and safe therapy for the treatment of T2DM since last decade. In order to design novel DPP-4 inhibitors, various in silico studies such as 3D-QSAR, pharmacophore modeling and virtual screening were performed and on the basis of the combined results of them, total 50 triazolo[5,1-c][1,2,4]triazine derivatives were designed and mapped on the best pharmacophore model...
March 6, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28296924/changes-in-surface-glycosylation-and-glycocalyx-shedding-in-trichobilharzia-regenti-schistosomatidae-during-the-transformation-of-cercaria-to-schistosomulum
#6
Jana Řimnáčová, Libor Mikeš, Libuše Turjanicová, Jana Bulantová, Petr Horák
The invasive larvae (cercariae) of schistosomes penetrate the skin of their definitive hosts. During the invasion, they undergo dramatic ultrastructural and physiological transitions. These changes result in the development of the subsequent stage, schistosomulum, which migrates through host tissues in close contact with host's immune system. One of the striking changes in the transforming cercariae is the shedding of their thick tegumental glycocalyx, which represents an immunoattractive structure; therefore its removal helps cercariae to avoid immune attack...
2017: PloS One
https://www.readbyqxmd.com/read/28296349/dipeptidyl-peptidase-4-inhibitors-as-preferable-oral-hypoglycemic-agents-in-terms-of-treatment-satisfaction-results-from-a-multicenter-12-week-open-label-randomized-controlled-study-in-japan
#7
Hitoshi Ishii, Yasuaki Hayashino, Yasuhiro Akai, Matahiro Yabuta, Satoru Tsujii
AIMS/INTRODUCTION: To compare the treatment satisfaction of four classes of oral hypoglycemic agents (OHAs): dipeptidyl peptidase-4 (DPP-4) inhibitors, α-glucosidase inhibitors (αGI), biguanides (BG), and sulfonylureas (SU), which are common initial treatments for type 2 diabetes mellitus patients in Japan, and to identify the best OHA in terms of treatment satisfaction. MATERIALS AND METHODS: In this 12-week, randomized, controlled, open-label study, Japanese outpatients with type 2 diabetes mellitus who were naïve to pharmacological treatment were randomly assigned a DPP-4 inhibitor, a BG, an αGI, or a SU...
March 14, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/28295491/national-trends-in-the-treatment-of-diabetic-nephropathy-in-the-united-states
#8
O Ajiboye, J B Segal
WHAT IS KNOWN AND OBJECTIVE: The prevalence of diabetic nephropathy continues to rise and it remains a strong predictor of morbidity and mortality in diabetic patients. Patients diagnosed with diabetic nephropathy are actively excluded from most trials involving diabetic medications and it is important to understand the prescription patterns in this subset of patients with diabetes. METHODS: Using the IMS Health's National Disease and Therapeutic Index, we analysed the medication prescription patterns for six classes of medications from 2010 to 2014 among patients, 35 years or older, with diabetic nephropathy...
March 15, 2017: Journal of Clinical Pharmacy and Therapeutics
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/28292575/the-treatment-of-type-2-diabetes-mellitus-in-patients-with-chronic-kidney-disease-what-to-expect-from-new-oral-hypoglycemic-agents
#10
REVIEW
Luca Di Lullo, Michela Mangano, Claudio Ronco, Vincenzo Barbera, Antonio De Pascalis, Antonio Bellasi, Domenico Russo, Biagio Di Iorio, Mario Cozzolino
Worldwide, an estimated 200 million people have chronic kidney disease (CKD), whose most common causes include hypertension, arteriosclerosis, and diabetes. About 40% of patients with diabetes develop CKD and intensive blood glucose control through pharmacological intervention can delay CKD progression. Standard therapies for the treatment of type 2 diabetes mellitus include metformin, sulfonylureas, meglitinides, thiazolidinediones, and insulin. While these drugs have an important role in the management of type 2 diabetes, only the thiazolidinedione pioglitazone can be used across the spectrum of CKD (stages 2-5) and without dose adjustment...
March 6, 2017: Diabetes & Metabolic Syndrome
https://www.readbyqxmd.com/read/28291655/the-cardiovascular-safety-trials-of-dpp-4-inhibitors-glp-1-agonists-and-sglt2-inhibitors
#11
REVIEW
Matthew H Secrest, Jacob A Udell, Kristian B Filion
In this paper, we review the results of large, double-blind, placebo-controlled randomized trials mandated by the US Food and Drug Administration to examine the cardiovascular safety of newly-approved antihyperglycemic agents in patients with type 2 diabetes. The cardiovascular effects of dipeptidyl peptidase-4 (DPP-4) inhibitors remain controversial: while these drugs did not reduce or increase the risk of primary, pre-specified composite cardiovascular outcomes, one DPP-4 inhibitor (saxagliptin) increased the risk of hospitalization for heart failure in the overall population; another (alogliptin) demonstrated inconsistent effects on heart failure hospitalization across subgroups of patients, and a third (sitagliptin) demonstrated no effect on heart failure...
January 28, 2017: Trends in Cardiovascular Medicine
https://www.readbyqxmd.com/read/28291027/estrogen-and-dpp-4-inhibitor-share-similar-efficacy-in-reducing-brain-pathology-caused-by-cardiac-ischemia-reperfusion-injury-in-both-lean-and-obese-estrogen-deprived-rats
#12
Wasana Pratchayasakul, Sivaporn Sivasinprasasn, Piangkwan Sa-Nguanmoo, Cicely Proctor, Sasiwan Kerdphoo, Nipon Chattipakorn, Siriporn C Chattipakorn
OBJECTIVE: Cardiac ischemia-reperfusion injury (I/R) caused an oxidative burst, increased beta-amyloid production, and decreased dendritic spine density in the brain. However, the effect of cardiac I/R in the brain of estrogen-deprived rats who were or were not obese have not been investigated. Moreover, the benefits of estrogen or dipeptidyl peptidase-4 (DDP-4) inhibitor therapies in those conditions have never been determined. We hypothesized that cardiac I/R aggravates brain pathology in estrogen-deprived obese rats, to a greater extent when compared with estrogen-deprived lean rats, and treatment with either estrogen or a DPP-4 inhibitor attenuates those adverse effects...
March 13, 2017: Menopause: the Journal of the North American Menopause Society
https://www.readbyqxmd.com/read/28290283/ace-inhibitory-peptides-from-bovine-caseins-released-with-peptidases-from-maclura-pomifera-latex
#13
María Alicia Corrons, Constanza Silvina Liggieri, Sebastián Alejandro Trejo, Mariela Anahí Bruno
In work reported here, a proteolytic extract prepared from Maclura pomifera latex was employed to hydrolyze bovine caseins. Densitograms of Tricine-sodium-dodecyl-sulfate-polyacrylamide-gel electrophoresis (SDS-PAGE) indicated that the caseins were considerably degraded after a 10-min reaction. The degree of hydrolysis determined by the 2,4,6-trinitrobenzenesulfonic-acid method was 17.1±0.7% after 180min of digestion. The concentration of small peptides increased with hydrolysis time, and analysis by reverse-phase high-performance liquid chromatography (RP HPLC) and mass spectrometry, revealed a virtually unchanged peptide profile...
March 2017: Food Research International
https://www.readbyqxmd.com/read/28288492/correlating-in-vitro-target-oriented-screening-and-docking-inhibition-of-matrix-metalloproteinases-activities-by-flavonoids
#14
Lucia Crascì, Livia Basile, Annamaria Panico, Carmelo Puglia, Francesco P Bonina, Pierluigi Maria Basile, Luisa Rizza, Salvatore Guccione
Metalloproteases are a family of zinc-containing endopeptidases involved in a variety of pathological disorders. The use of flavonoid derivatives as potential metalloprotease inhibitors has recently increased.Particular plants growing in Sicily are an excellent yielder of the flavonoids luteolin, apigenin, and their respective glycoside derivatives (7-O-rutinoside, 7-O-glucoside, and 7-O-glucuronide).The inhibitory activity of luteolin, apigenin, and their respective glycoside derivatives on the metalloproteases MMP-1, MMP-3, MMP-13, MMP-8, and MMP-9 was assessed and rationalized correlating in vitro target-oriented screening and in silico docking...
March 13, 2017: Planta Medica
https://www.readbyqxmd.com/read/28288130/parl-mediates-smac-proteolytic-maturation-in-mitochondria-to-promote-apoptosis
#15
Shotaro Saita, Hendrik Nolte, Kai Uwe Fiedler, Hamid Kashkar, A Saskia Venne, René P Zahedi, Marcus Krüger, Thomas Langer
Mitochondria drive apoptosis by releasing pro-apoptotic proteins that promote caspase activation in the cytosol. The rhomboid protease PARL, an intramembrane cleaving peptidase in the inner membrane, regulates mitophagy and plays an ill-defined role in apoptosis. Here, we employed PARL-based proteomics to define its substrate spectrum. Our data identified the mitochondrial pro-apoptotic protein Smac (also known as DIABLO) as a PARL substrate. In apoptotic cells, Smac is released into the cytosol and promotes caspase activity by inhibiting inhibitors of apoptosis (IAPs)...
March 13, 2017: Nature Cell Biology
https://www.readbyqxmd.com/read/28285800/perspectives-on-cardiovascular-effects-of-incretin-based-drugs-from-bedside-to-bench-return-trip
#16
Michaela Luconi, Giulia Cantini, Antonio Ceriello, Edoardo Mannucci
Recently, cardiovascular outcome trials with glucose-lowering drugs used in type 2 diabetes mellitus, namely glucagon-like peptide-1 receptor agonists (GLP-1RA), liraglutide and semaglutide, showed a reduction in cardiovascular events, which had not been observed in trials with other incretin-based drugs, such as lixisenatide or with dipeptidyl peptidase-4 inhibitors (DPP4i). Mechanisms underlying the observed cardiovascular differences between DPP4i and GLP1-RA, and across individual GLP1-RA are poorly understood...
March 2, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28285415/naag-peptidase-inhibitors-act-via-mglur3-animal-models-of-memory-alzheimer-s-and-ethanol-intoxication
#17
Rafal T Olszewski, Karolina J Janczura, Tomasz Bzdega, Elise K Der, Faustino Venzor, Brennen O'Rourke, Timothy J Hark, Kirsten E Craddock, Shankar Balasubramanian, Charbel Moussa, Joseph H Neale
Glutamate carboxypeptidase II (GCPII) inactivates the peptide neurotransmitter N-acetylaspartylglutamate (NAAG) following synaptic release. Inhibitors of GCPII increase extracellular NAAG levels and are efficacious in animal models of clinical disorders via NAAG activation of a group II metabotropic glutamate receptor. mGluR2 and mGluR3 knock-out (ko) mice were used to test the hypothesis that mGluR3 mediates the activity of GCPII inhibitors ZJ43 and 2-PMPA in animal models of memory and memory loss. Short- (1...
March 11, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28284167/albiglutide-for-the-treatment-of-type-2-diabetes-mellitus-an-integrated-safety-analysis-of-the-harmony-phase-3-trials
#18
Bo Ahrén, Molly C Carr, Karen Murphy, Christopher Perkins, Marc Rendell, Jason Mallory, Timothy Wilson, Susan Johnson
AIMS: Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) stimulate the incretin system and lower glycaemic parameters in type 2 diabetes mellitus (T2DM). This analysis of clinical studies of up to 3years evaluated the safety of albiglutide, a GLP-1 RA, in people with T2DM. METHODS: Integrated safety analysis included seven phase-3 T2DM studies of albiglutide compared with placebo and/or active comparators (a dipeptidyl peptidase-4 inhibitor, GLP-1 RA, insulin, sulphonylurea, and thiazolidinedione)...
February 20, 2017: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28281660/dpp-4-inhibitor-and-estrogen-share-similar-efficacy-against-cardiac-ischemic-reperfusion-injury-in-obese-insulin-resistant-and-estrogen-deprived-female-rats
#19
Sivaporn Sivasinprasasn, Pongpan Tanajak, Wanpitak Pongkan, Wasana Pratchayasakul, Siriporn C Chattipakorn, Nipon Chattipakorn
Estrogen deprivation aggravates cardiac injury after myocardial ischemia and reperfusion (I/R) injury. Although either estrogen or the dipeptidyl peptidase-4 (DPP-4) inhibitor, vildagliptin, reduces myocardial damage following cardiac I/R, their effects on the heart in obese-insulin resistant and estrogen deprived conditions remain unknown. Ovariectomized (O) rats (n = 36) were divided to receive either normal diet (NDO) or high-fat diet (HFO) for 12 weeks, followed by treatment with a vehicle, estrogen or vildagliptin for 4 weeks...
March 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28276972/pharmacotherapy-of-treatment-resistant-type-2-diabetes
#20
André J Scheen
Despite type 2 diabetes (T2D) management offers a variety of pharmacological interventions targeting different defects, numerous patients remain with persistent hyperglycaemia responsible for severe complications. Unlike resistant hypertension, treatment resistant T2D is not a classical concept although it is a rather common observation in clinical practice. Areas covered: This article proposes a definition for 'treatment resistant diabetes', analyses the causes of poor glucose control despite standard therapy, briefly considers the alternative approaches to glucose-lowering pharmacotherapy and finally describes how to overcome poor glycaemic control, using innovative oral or injectable combination therapies...
March 1, 2017: Expert Opinion on Pharmacotherapy
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