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dipeptidyl peptidase 4

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https://www.readbyqxmd.com/read/28094469/immunohistochemical-assessment-of-glucagon-like-peptide-1-receptor-glp-1r-expression-in-the-pancreas-of-patients-with-type-2-diabetes
#1
Rikke Kaae Kirk, Charles Pyke, Matthias G von Herrath, Jane Preuss Hasselby, Lars Pedersen, Pia Gottrup Mortensen, Lotte Bjerre Knudsen, Ken Coppieters
Glucagon-like peptide-1 (GLP-1) is an incretin hormone which stimulates insulin release and inhibits glucagon secretion from the pancreas in a glucose-dependent manner. Incretin-based therapies, consisting of GLP-1 receptor (GLP-1R) agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors, are used for the treatment of T2D. Immunohistochemical studies for GLP-1R expression have previously been hampered by the use of unspecific polyclonal antibodies. This study used a new monoclonal antibody to assess GLP-1R expression in pancreatic tissue from 23 patients with T2D, including 7 with a DPP-4 inhibitor and 1 with a GLP-1R agonist treatment history...
January 17, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28093996/challenges-related-to-glycemic-control-in-type-2-diabetes-mellitus-patients
#2
Masoumeh Kheirandish, Hamidreza Mahboobi, Maryam Yazdanparast, Mohammad Amjad Kamal
Diabetes mellitus (DM) is a chronic disease with long-term complications. Glycemic control is an important part in management of DM. The first line in treatment of type 2 DM (T2DM) is diet and life style change. Metformin is the first choice of medication in T2DM patients. Sulfonylureas have high risk of hypoglycemia. Glinides are associated with lower risk of hypoglycemia in comparison to sulfonylureas. Also α-glucosidase inhibitors decrease the polysacarides digestion in small intestine and less effective in comparison to metformin and sulfonylureas in lowering hemoglobin A1c (HbA1c)...
January 15, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28093853/randomized-clinical-trial-comparing-the-efficacy-and-safety-of-treatment-with-the-once-weekly-dipeptidyl-peptidase-4-dpp-4-inhibitor-omarigliptin-or-the-once-daily-dpp-4-inhibitor-sitagliptin-in-patients-with-type-2-diabetes-inadequately-controlled-on-metformin
#3
Ronald Goldenberg, Ira Gantz, Paula J Andryuk, Edward A O'Neill, Keith D Kaufman, Eseng Lai, Yin Na Wang, Shailaja Suryawanshi, Samuel S Engel
AIM: To compare the efficacy and safety of the once-weekly oral dipeptidyl peptidase-4 (DPP-4) inhibitor omarigliptin or once-daily DPP-4 inhibitor sitagliptin in patients with type 2 diabetes (T2DM) and inadequate glycaemic control on metformin. MATERIALS AND METHODS: Patients with T2DM with a glycated haemoglobin (HbA1c) concentration ≥6.5% to ≤9.0% while on a stable dose of metformin (≥1500 mg/d) were randomized in a double-blind manner to receive omarigliptin 25 mg once weekly (n = 322) or sitagliptin 100 mg once daily (n = 320)...
January 17, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28093794/design-synthesis-and-biological-evaluation-of-novel-quinazoline-clubbed-thiazoline-derivatives
#4
Zulphikar Ali, Md J Akhtar, Anees A Siddiqui, Ahsan A Khan, Md R Haider, Mohammad S Yar
A novel series of quinazoline clubbed thiazoline derivatives was rationally designed and synthesized. The newly synthesized compounds were evaluated for in vitro dipeptidyl peptidase IV (DPP-4) inhibitory activity. Compounds that showed good to moderate activity were compared using linagliptin as standard. Compound 4x (IC50  = 1.12 nM) exhibited the most promising results. The special chemical feature of compound 4x also imparts good inhibition selectivity for DPP-4 over DPP-8/9. Moreover, docking of compound 4x into the active site of DPP-4 illustrates its possible binding interactions...
January 17, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28091829/inhibition-of-dpp-4-activity-and-neuronal-atrophy-with-genistein-attenuates-neurological-deficits-induced-by-transient-global-cerebral-ischemia-and-reperfusion-in-streptozotocin-induced-diabetic-mice
#5
Mithun Singh Rajput, Purnima Dey Sarkar, Nilesh Prakash Nirmal
Genistein, an isoflavonoid phytoestrogen, has been known for its potential pharmacological properties especially for neuroprotection and treating diabetes. The present study aims to determine the neuroprotective efficacy of genistein against global cerebral ischemia-reperfusion-induced neuronal injury in streptozotocin-induced diabetic mice and explore the underlying mechanisms. Streptozotocin-induced diabetic mice were subjected to transient cerebral ischemia by occluding both common carotid arteries for 30 min followed by 24 h reperfusion to induce neuronal injury...
January 16, 2017: Inflammation
https://www.readbyqxmd.com/read/28086872/dapagliflozin-decreases-small-dense-low-density-lipoprotein-cholesterol-and-increases-high-density-lipoprotein-2-cholesterol-in-patients-with-type-2-diabetes-comparison-with-sitagliptin
#6
Toshiyuki Hayashi, Tomoyasu Fukui, Noriko Nakanishi, Saki Yamamoto, Masako Tomoyasu, Anna Osamura, Makoto Ohara, Takeshi Yamamoto, Yasuki Ito, Tsutomu Hirano
BACKGROUND: The sodium-glucose co-transporter-2 (SGLT-2) inhibitors have been reported to increase both low-density lipoprotein (LDL) and high-density lipoprotein (HDL)-cholesterol (C). This study aimed to determine how SGLT-2 inhibitors affect LDL and HDL-C subspecies. METHODS: This single center, open-label, randomized, prospective study included 80 patients with type 2 diabetes taking prescribed oral hypoglycemic agents. Patients were allocated to receive dapagliflozin (n = 40) or sitagliptin (n = 40) as add-on treatment...
January 13, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28078647/sitagliptin-a-review-in-type-2-diabetes
#7
Lesley J Scott
The dipeptidyl peptidase-4 inhibitor sitagliptin (Januvia(®); Glactiv(®); Tesavel(®); Xelevia™) is approved in more than 130 countries worldwide as monotherapy and in combination with other antihyperglycaemic drugs for the treatment of adult patients with type 2 diabetes (T2D). Extensive clinical experience has firmly established the glycaemic efficacy of oral sitagliptin (±other antihyperglycaemic drugs) in a broad spectrum of patients with T2D, including obese, elderly and renally impaired patients and those with established cardiovascular (CV) disease (CVD)...
January 11, 2017: Drugs
https://www.readbyqxmd.com/read/28077733/identification-of-potential-plasma-biomarkers-for-nonalcoholic-fatty-liver-disease-by-integrating-transcriptomics-and-proteomics-in-laying-hens
#8
Meng-Tsz Tsai, Yu-Jen Chen, Ching-Yi Chen, Mong-Hsun Tsai, Chia-Li Han, Yu-Ju Chen, Harry J Mersmann, Shih-Torng Ding
BACKGROUND: Prevalent worldwide obesity is associated with increased incidence of nonalcoholic fatty liver disease (NAFLD) and metabolic syndrome. The identification of noninvasive biomarkers for NAFLD is of recent interest. Because primary de novo lipogenesis occurs in chicken liver as in human liver, adult chickens with age-associated steatosis resembling human NAFLD is an appealing animal model. OBJECTIVE: The objective of this study was to screen potential biomarkers in the chicken model for NAFLD by transcriptomic and proteomic analysis...
January 11, 2017: Journal of Nutrition
https://www.readbyqxmd.com/read/28065853/sitagliptin-inhibit-human-lymphocytes-proliferation-and-th1-th17-differentiation-in-vitro
#9
Marcelo Maia Pinheiro, Caroline Lais Stoppa, Claudete Justina Valduga, Cristina Eunice Okuyama, Renata Gorjão, Regina Mara Silva Pereira, Susana Nogueira Diniz
Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of anti-diabetic agents that are widely used in clinical practice to improve glycemic control in patients with type 2 diabetes. DPP-4 is also known as lymphocyte cell surface protein, CD26, and plays an important role in T-cell immunity. Recent studies suggest that DPP-4 inhibitors improve beta-cell function and attenuate autoimmunity in type 1 diabetic mouse models. To investigate the direct effect of DPP4 in immune response, human peripheral blood mononuclear cells (PBMC) from healthy volunteers were obtained by Ficoll gradient and cultivated in the absence (control) or presence of phytohemagglutinin (PHA), or stimulated with PHA and treated with sitagliptin...
January 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28058753/effect-of-gemigliptin-on-glycemic-variability-in-patients-with-type-2-diabetes
#10
Se E Park, Byung W Lee, Jae H Kim, Woo J Lee, Jae H Cho, Chang H Jung, Seung H Lee, Sunghwan Suh, Gwong C Hur, Sung H Kim, Young H Jang, Cheol Y Park
The aim of this study was to evaluate the effect of gemigliptin vs sitagliptin or glimepiride as initial combination therapy with metformin on glycemic variability and to assess the correlation between glycemic variability reduction and the dipeptidyl peptidase-4 (DPP-4) inhibition in patients with type 2 diabetes. This multicenter, randomized, active-controlled, open-label exploratory study included 69 patients with HbA1c >7.5%. Subjects were randomized to receive gemigliptin 50 mg (n = 24), sitagliptin 100 mg (n = 23), or glimepiride 2 mg (n = 22) for 12 weeks...
January 6, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28058750/efficacy-and-safety-of-adding-evogliptin-versus-sitagliptin-in-metformin-treated-patients-with-type-2-diabetes-a-24-week-randomised-controlled-trial-with-open-label-extension
#11
Sang-Mo Hong, Cheol-Young Park, Dong-Min Hwang, Kyung Ah Han, Chang Beom Lee, Choon Hee Chung, Kun-Ho Yoon, Ji-Oh Mok, Kyong Soo Park, Sung-Woo Park
AIMS: This trial consisted of a 24-week multicenter, randomised, double-blind, double-dummy, active-controlled study and a 52-week open label extension study to assess the efficacy and safety of evogliptin, a novel dipeptidyl peptidase-4 inhibitor, compared to sitagliptin in patients with type 2 diabetes who have inadequate glycaemic control with metformin alone. MATERIALS AND METHODS: Adult type 2 diabetes mellitus patients (N = 222) with HbA1c 6.5-11% on stable metformin doses (≥1000 mg/day) were randomised 1:1 to add-on 5 mg evogliptin (N = 112) or 100 mg sitagliptin (N = 110) once daily for 24 weeks...
January 6, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28056431/second-line-initiation-of-insulin-compared-with-dpp-4-inhibitors-after-metformin-monotherapy-is-associated-with-increased-risk-of-all-cause-mortality-cardiovascular-events-and-severe-hypoglycemia
#12
Thomas Nyström, Johan Bodegard, David Nathanson, Marcus Thuresson, Anna Norhammar, Jan W Eriksson
AIMS: The objective of this nationwide study was to compare the risk of all-cause mortality, fatal and nonfatal cardiovascular disease (CVD), and severe hypoglycemia in patients with type 2 diabetes (T2D) on metformin monotherapy treatment starting second-line treatment with either insulin or dipeptidyl peptidase-4 inhibitor (DPP-4i). METHODS: All patients with T2D in Sweden who initiated second-line treatment with insulin or DPP-4i after metformin monotherapy during 2007-2014 identified in the Swedish Prescribed Drug Register were followed for outcome in the Cause of Death and National Patient Registers...
December 19, 2016: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28056430/the-effects-of-sitagliptin-a-dpp-4-inhibitor-on-cognitive-functions-in-elderly-diabetic-patients-with-or-without-alzheimer-s-disease
#13
Ahmet Turan Isik, Pinar Soysal, Adnan Yay, Cansu Usarel
AIMS: The present study aimed to evaluate effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor (DPP-4I), on cognitive functions in elderly diabetic patients with and without cognitive impairment. METHODS: 253 elderly patients with type 2DM, were enrolled in this prospective and observational study. After comprehensive geriatric assessment, the patients were divided into either sitagliptin or non-sitagliptin group. RESULTS: A total of 205 patients who completed the study (52 with Alzheimer's Disease (AD)) were re-evaluated 6months later...
December 21, 2016: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28055075/oral-pharmacologic-treatment-of-type-2-diabetes-mellitus-a-clinical-practice-guideline-update-from-the-american-college-of-physicians
#14
Amir Qaseem, Michael J Barry, Linda L Humphrey, Mary Ann Forciea
Description: The American College of Physicians (ACP) developed this guideline to present the evidence and provide clinical recommendations on oral pharmacologic treatment of type 2 diabetes in adults. This guideline serves as an update to the 2012 ACP guideline on the same topic. This guideline is endorsed by the American Academy of Family Physicians. Methods: This guideline is based on a systematic review of randomized, controlled trials and observational studies published through December 2015 on the comparative effectiveness of oral medications for type 2 diabetes...
January 3, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28039605/pharmacokinetic-characteristics-and-clinical-efficacy-of-an-sglt2-inhibitor-plus-dpp-4-inhibitor-combination-therapy-in-type-2-diabetes
#15
REVIEW
André J Scheen
Type 2 diabetes (T2D) generally requires a combination of several pharmacological approaches to control hyperglycaemia. Combining a sodium-glucose cotransporter type 2 inhibitor (SGLT2I, also known as gliflozin) and a dipeptidyl peptidase-4 inhibitor (DPP-4I, also known as gliptin) appears to be an attractive strategy because of complementary modes of action. This narrative review analyzes the pharmacokinetics and clinical efficacy of different combined therapies with an SGLT2I (canagliflozin, dapagliflozin, empagliflozin, ertugliflozin, ipragliflozin, luseogliflozin, tofogliflozin) and DPP-4I (linagliptin, saxagliptin, sitagliptin, teneligliptin)...
December 30, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28039172/toward-defining-the-threshold-between-low-and-high-glucose-variability-in-diabetes
#16
Louis Monnier, Claude Colette, Anne Wojtusciszyn, Sylvie Dejager, Eric Renard, Nicolas Molinari, David R Owens
OBJECTIVE: To define the threshold for excess glucose variability (GV), one of the main features of dysglycemia in diabetes. RESEARCH DESIGN AND METHODS: A total of 376 persons with diabetes investigated at the University Hospital of Montpellier (Montpellier, France) underwent continuous glucose monitoring. Participants with type 2 diabetes were divided into several groups-groups 1, 2a, 2b, and 3 (n = 82, 28, 65, and 79, respectively)-according to treatment: 1) diet and/or insulin sensitizers alone; 2) oral therapy including an insulinotropic agent, dipeptidyl peptidase 4 inhibitors (group 2a), or sulfonylureas (group 2b); or 3) insulin...
December 30, 2016: Diabetes Care
https://www.readbyqxmd.com/read/28029729/combination-treatment-of-dipeptidyl-peptidase-iv-inhibitor-sitagliptin-and-angiotensin-ii-type-1-receptor-blocker-losartan-suppresses-progression-in-a-nondiabetic-rat-model-of-steatohepatitis
#17
Yasushi Okura, Tadashi Namisaki, Kei Moriya, Mitsuteru Kitade, Kosuke Takeda, Kosuke Kaji, Ryuichi Noguchi, Norihisa Nishimura, Kenichiro Seki, Hideto Kawaratani, Hiroaki Takaya, Shinya Sato, Yasuhiko Sawada, Naotaka Shimozato, Masanori Furukawa, Keisuke Nakanishi, Saikawa Soichiro, Takuya Kubo, Kiyoshi Asada, Hitoshi Yoshiji
AIM: Dipeptidyl peptidase-4 (DPP4) inhibitors (DPP4-I) are oral glucose-lowering drugs for type 2 diabetes mellitus. Previously, we demonstrated that DPP4-I (sitagliptin) exerted suppressive effects on experimental liver fibrosis in rats. Blockade of the renin-angiotensin system by angiotensin-II type 1 receptor blocker (ARB: losartan), commonly used in the management of hypertension, has been shown to significantly alleviate hepatic fibrogenesis and carcinogenesis. We aimed to elucidate the effects and possible mechanisms of a sitagliptin + losartan combination on the progression of nondiabetic nonalcoholic steatohepatitis (NASH) in a rat model...
December 28, 2016: Hepatology Research: the Official Journal of the Japan Society of Hepatology
https://www.readbyqxmd.com/read/28027711/molecular-modeling-and-statistical-analysis-in-the-design-of-derivatives-of-human-dipeptidyl-peptidase-iv
#18
Alison L E Pereira, Gabriela B Dos Santos, Márcia S F Franco, Leonardo B Federico, Carlos H T P da Silva, Cleydson B R Santos
Human Dipeptidyl Peptidase IV (hDDP-IV) has a considerable importance in inactivation of glucagon-like peptide-1 (GLP-1), which is related to type 2 diabetes. One approach for the treatment is the development of small hDDP-IV inhibitors. In order to design better inhibitors, we analyzed 5-(aminomethyl)-6-(2,4-dichlrophenyl)-2-(3,5-dimethoxyphenyl)pyrimidin-4-amine and a set of 24 molecules found in the BindingDB web database for model designing. The analysis of their molecular properties allowed the design of a Multiple Linear Regression Model for activity prediction...
December 28, 2016: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28027447/dynamic-compound-dependent-acoustic-transfer-to-investigate-inhibitor-reversibility
#19
Jennifer Nothstein, Elisabeth MacColl, Paul Zuck, Jason Cassaday, Victor N Uebele, Jeffrey D Hermes, Michelle F Homsher
Automated mechanism of action studies are introducing the need for tailored compound delivery, which can be challenging for standard compound management procedures. Jump dilution assays investigating inhibitor reversibility require compound delivery at specific volumes to assay specific concentrations of 10 × IC50 for each inhibitor. Creating custom-made source plates with unique compound concentrations to dispense a uniform single volume can be prohibitively slow. A broadly applicable tool that enables on-the fly dispensing of variable amounts of stock concentrations was developed using the Acoustic Transfer System (ATS)...
December 1, 2016: Journal of Laboratory Automation
https://www.readbyqxmd.com/read/28026912/efficacy-and-safety-of-gemigliptin-a-dipeptidyl-peptidase-4-inhibitor-in-patients-with-type-2-diabetes-mellitus-inadequately-controlled-with-combination-treatment-of-metformin-and-sulfonylurea-a-24-week-multicenter-randomized-double-blind-placebo-controlled
#20
Chang Ho Ahn, Kyung Ah Han, Jae Myung Yu, Joo Young Nam, Kyu Jeung Ahn, Tae Keun Oh, Hyoung Woo Lee, Dae Ho Lee, Jaetaek Kim, Choon Hee Chung, Tae Sun Park, Byung Joon Kim, Seok Won Park, Hyeong Kyu Park, Kwang Jae Lee, Sang-Wook Kim, Jeong Hyun Park, Kwan Pyo Ko, Chong Hwa Kim, Hyunjin Lee, Hak Chul Jang, Kyong Soo Park
AIMS: To assess the efficacy and safety of gemigliptin, a dipeptidyl peptidase-4 inhibitor, added to metformin and sulfonylurea in patients with type 2 diabetes. MATERIALS AND METHODS: We conducted a randomized, double-blind, placebo-controlled trial in 219 Korean patients inadequately controlled with metformin and glimepiride. Patients were randomized to gemigliptin 50 mg once daily or placebo added to metformin and glimepiride. The primary endpoint was the change in hemoglobin A1c (HbA1c) from baseline to week 24...
December 27, 2016: Diabetes, Obesity & Metabolism
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