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Dipeptidyl peptidase

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https://www.readbyqxmd.com/read/29777520/relationship-of-eating-patterns-and-metabolic-parameters-and-teneligliptin-treatment-interim-results-from-post-marketing-surveillance-in-japanese-type-2-diabetes-patients
#1
Takashi Kadowaki, Masakazu Haneda, Hiroshi Ito, Kazuyo Sasaki, Sonoe Hiraide, Miyuki Matsukawa, Makoto Ueno
INTRODUCTION: Healthy eating is a critical aspect of the prevention and management of type 2 diabetes (T2DM). Disrupted eating patterns can result in poor glucose control and increase the likelihood of diabetic complications. Teneligliptin inhibits dipeptidyl peptidase-4 activity for 24 h and suppresses postprandial hyperglycemia after all three daily meals. This interim analysis of data from the large-scale post-marketing surveillance of teneligliptin (RUBY) in Japan examined eating patterns and their relationship with metabolic parameters and diabetic complications...
May 17, 2018: Advances in Therapy
https://www.readbyqxmd.com/read/29776406/the-effect-of-dpp-4-inhibition-to-improve-functional-outcome-after-stroke-is-mediated-by-the-sdf-1%C3%AE-cxcr4-pathway
#2
Fausto Chiazza, Harald Tammen, Hiranya Pintana, Grazyna Lietzau, Massimo Collino, Thomas Nyström, Thomas Klein, Vladimer Darsalia, Cesare Patrone
BACKGROUND: Dipeptidyl peptidase-4 (DPP-4) inhibitors (gliptins) are approved drugs for the treatment of hyperglycemia in patients with type 2 diabetes. These effects are mainly mediated by inhibiting endogenous glucagon-like peptide-1 (GLP-1) cleavage. Interestingly, gliptins can also improve stroke outcome in rodents independently from GLP1. However, the underlying mechanisms are unknown. Stromal cell-derived factor-1α (SDF-1α) is a DPP-4 substrate and CXCR4 agonist promoting beneficial effects in injured brains...
May 19, 2018: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/29774053/postherpes-simplex-encephalitis-a-case-series-of-viral-triggered-autoimmunity-synaptic-autoantibodies-and-response-to-therapy
#3
Harry Alexopoulos, Sofia Akrivou, Sotiria Mastroyanni, Maria Antonopoulou, Argirios Dinopoulos, Melpo Giorgi, Kostas Konstantinou, Evangelos Kouremenos, Maria Lariou, Dimitrios Naoumis, Efterpi Pavlidou, Evaggelos Pavlou, Konstantinos Voudris, Panayotis Vlachoyiannopoulos, Marinos C Dalakas
Background: Recent evidence suggests that patients with herpes simplex virus (HSV) encephalitis may relapse because of autoimmunity against the N-methyl-D-aspartate receptor (NMDAR). We present a case series of post-HSV relapsing encephalopathy associated with antibodies to central nervous system (CNS) synaptic antigens. Patient/Methods: Sera and cerebrospinal fluid (CSF) from five patients with HSV encephalitis who relapsed after antiviral therapy were tested for anti-NMDAR, gamma-aminobutyric acid b receptor (GABAbR), α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR), Leucine-rich, glioma inactivated 1 (LGI1), anti -contactin-associated protein-like 2 (CASPR2) and dipeptidyl-peptidase-like protein-6 (DDPX) antibodies using cell-based assays...
2018: Therapeutic Advances in Neurological Disorders
https://www.readbyqxmd.com/read/29773502/design-synthesis-and-biological-evaluation-of-novel-pyrimidinedione-derivatives-as-dpp-4-inhibitors
#4
Ning Li, Li-Jun Wang, Bo Jiang, Shu-Ju Guo, Xiang-Qian Li, Xue-Chun Chen, Jiao Luo, Chao Li, Yi Wang, Da-Yong Shi
A series of novel pyrimidinedione derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) inhibitory activity and in vivo anti-hyperglycemic efficacy. Among them, the representative compounds 11, 15 and 16 showed excellent inhibitory activity of DPP-4 with IC50 values of 64.47 nM, 188.7 nM and 65.36 nM, respectively. Further studies revealed that compound 11 was potent in vivo hypoglycemic effect. The structure-activity relationships of these pyrimidinedione derivatives had been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes...
May 14, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29772538/targeting-fibroblast-activation-protein-in-cancer-prospects-and-caveats
#5
Petr Busek, Rosana Mateu, Michal Zubal, Lenka Kotackova, Aleksi Sedo
Fibroblast activation protein (FAP, seprase) is a serine protease with post-proline dipeptidyl peptidase and endopeptidase enzymatic activity. FAP is upregulated in several tumor types, while its expression in healthy adult tissues is scarce. FAP molecule itself and FAP+ stromal cells play an important although probably context-dependent and tumor type-specific pathogenetic role in tumor progression. We provide an overview of FAP expression under both physiological and pathological conditions with focus on human malignancies...
June 1, 2018: Frontiers in Bioscience (Landmark Edition)
https://www.readbyqxmd.com/read/29772527/a-novel-role-for-cd26-dipeptidyl-peptidase-iv-as-a-therapeutic-target
#6
Kei Ohnuma, Ryo Hatano, Eriko Komiya, Haruna Otsuka, Takumi Itoh, Noriaki Iwao, Yutaro Kaneko, Taketo Yamada, Nam H Dang, Chikao Morimoto
CD26 is a 110 kDa surface glycoprotein with intrinsic dipeptidyl peptidase IV activity that is expressed on numerous cell types and has a multitude of biological functions. The role of CD26 in immune regulation has been extensively characterized, with recent findings elucidating its linkage with signaling pathways and structures involved in T-lymphocyte activation as well as antigen presenting cell-T-cell interaction. In this paper, we will review emerging data on CD26-mediated immune regulation suggesting that CD26 may be an appropriate therapeutic target for the treatment of selected immune disorders as well as Middle East respiratory syndrome coronavirus...
June 1, 2018: Frontiers in Bioscience (Landmark Edition)
https://www.readbyqxmd.com/read/29770541/effect-of-short-term-treatment-with-sitagliptin-or-glibenclamide-on-daily-glucose-fluctuation-in-drug-na%C3%A3-ve-japanese-patients-with-type-2-diabetes-mellitus
#7
Ryo Suzuki, Jun-Ichi Eiki, Takashi Moritoyo, Kenichi Furihata, Akira Wakana, Yukari Ohta, Shigeru Tokita, Takashi Kadowaki
AIMS: To compare the effect of a dipeptidyl peptidase-4 inhibitor (DPP4-i) and a sulfonylurea (SU) on daily glucose fluctuation in drug-naïve Japanese patients with type 2 diabetes mellitus (T2DM). MATERIALS AND METHODS: Fifty-three drug-naïve Japanese patients with T2DM (HbA1c of 7.0% to 9.0% and fasting plasma glucose of 6.1 mmol/L or higher) were randomly assigned to either sitagliptin 50 mg q.d. or glibenclamide 2.5 mg per day (given in divided doses) in a 1:1 ratio...
May 17, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29769203/early-and-chronic-dipeptidyl-peptidase-iv-inhibition-and-cardiovascular-events-in-patients-with-type-2-diabetes-mellitus-after-an-acute-coronary-syndrome-a-landmark-analysis-of-the-examine-trial
#8
Abhinav Sharma, Christopher P Cannon, William B White, Yuyin Liu, George L Bakris, William C Cushman, Faiez Zannad
BACKGROUND: Antihyperglycemic therapies may increase the risk of cardiovascular events including hospitalization for heart failure. There is a paucity of data evaluating the cardiovascular safety of antihyperglycemic therapies in the high-risk period following an acute coronary syndrome (ACS). METHODS AND RESULTS: The EXAMINE (Examination of Cardiovascular Outcomes with Alogliptin versus Standard of Care) trial randomized 5380 patients who were 15 to 90 days post ACS to the dipeptidyl dipeptidase-IV (DPP-IV) inhibitor alogliptin versus placebo; mean follow-up was 18 months...
May 16, 2018: Journal of the American Heart Association
https://www.readbyqxmd.com/read/29768061/structural-re-positioning-in-silico-molecular-modelling-oxidative-degradation-and-biological-screening-of-linagliptin-as-adenosine-3-receptor-adora3-modulators-targeting-hepatocellular-carcinoma
#9
Bassam M Ayoub, Yasmeen M Attia, Mahmoud S Ahmed
Chemical entities with structural diversity were introduced as candidates targeting adenosine receptor with different clinical activities, containing 3,7-dihydro-1H-purine-2,6-dione, especially adenosine 3 receptors (ADORA3). Our initial approach started with pharmacophore screening of ADORA3 modulators; to choose linagliptin (LIN), approved anti-diabetic drug as Dipeptidyl peptidase-4 inhibitors, to be studied for its modulating effect towards ADORA3. This was followed by generation, purification, analytical method development, and structural elucidation of oxidative degraded product (DEG)...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29766812/switching-dipeptidyl-peptidase-4-inhibitors-to-tofogliflozin-a-selective-inhibitor-of-sodium-glucose-cotransporter-2-improves-arterial-stiffness-evaluated-by-cardio-ankle-vascular-index-in-patients-with-type-2-diabetes
#10
Nobuhiro Tahara, Sho-Ichi Yamagish, Munehisa Bekki, Atsuko Tahara, Sachiyo Igata, Akihiro Honda, Yoichi Sugiyama, Tomohisa Nakamura, Jiahui Sun, Yuki Kumashiro, Takanori Matsui, Yoshihiro Fukumoto
BACKGROUND: We have found that anagliptin, a dipeptidyl peptidase-4 inhibitor (DPP-4) significantly ameliorates arterial stiffness in type 2 diabetes mellitus (T2DM) patients compared with an equivalent hypoglycemic agent, glimepiride. However, it remains unclear whether and how switching DPP-4 inhibitors to tofogliflozin, a selective inhibitor of sodium-glucose cotransporter 2 (SGLT2) improves arterial stiffness in T2DM patients. METHODS: Nineteen T2DM patients who had received DPP-4 inhibitors for at least 1 year were enrolled in this study...
May 15, 2018: Current Vascular Pharmacology
https://www.readbyqxmd.com/read/29766544/dipeptidyl-peptidase-4-inhibitor-use-is-associated-with-decreased-risk-of-fracture-in-patients-with-type-2-diabetes-a-population-based-cohort-study
#11
Wen-Hsuan Hou, Kai-Cheng Chang, Chung-Yi Li, Huang-Tz Ou
AIMS: To investigate the putative link between dipeptidyl peptidase-4 inhibitor (DPP-4i) use and the risk of fracture in patients with type 2 diabetes. METHODS: This propensity-score-matched population-based cohort study was performed between 2009 and 2013 on patients with type 2 diabetes who were stable metformin users. A total of 3,996 patients with type 2 diabetes used DPP-4i as a second-line antidiabetic drug. The same number of matched non-DPP-4i users were followed up until fracture occurrence, health insurance policy termination, or the end of 2013...
May 16, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29766510/ineffectiveness-of-saxagliptin-as-a-neuroprotective-drug-in-6-ohda-lesioned-rats
#12
Joelle de Melo Turnes, Taysa Bervian Bassani, Leonardo C Souza, Maria A B F Vital
OBJECTIVES: To determine whether the drug saxagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor which is utilized for the treatment of Diabetes Mellitus, has neuroprotective effects in the animal model of Parkinson's disease (PD) induced by 6-hydroxydopamine (6-OHDA) in rats. METHODS: Male Wistar rats (weighing 280-300 g) received a bilateral infusion of 6-OHDA in the substantia nigra. Twenty-four hours later, they were treated with saxagliptin (1 mg/kg, p.o) once daily, for 21 days...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29764719/potential-use-of-bitter-melon-momordica-charantia-derived-compounds-as-antidiabetics-in-silico-and-in-vivo-studies
#13
Olusola Olalekan Elekofehinti, Esther Opeyemi Ariyo, Moses Orimoloye Akinjiyan, Olanrewaju Sam Olayeriju, Akeem Olalekan Lawal, Isaac Gbadura Adanlawo, Joao Batista Teixeira Rocha
Momordica charantia (bitter lemon) belongs to the cucurbitaceae family which has been extensively used in traditional medicines for the cure of various ailments such as cancer and diabetes. The underlying mechanism of M. charantia to maintain glycemic control was investigated. GLP-1 and DPP-4 gene modulation by M. charantia (5-20% inclusion in rats diet) was investigated in vivo by RT-PCR and possible compounds responsible for diabetic action predicted through in silico approach. Phytochemicalss previously characterized from M...
May 12, 2018: Pathophysiology: the Official Journal of the International Society for Pathophysiology
https://www.readbyqxmd.com/read/29763999/clinical-markers-associated-with-glycemic-response-to-dipeptidyl-peptidase-4-inhibitor-therapy
#14
Sho-Ichi Yamagishi
No abstract text is available yet for this article.
May 15, 2018: Diabetes/metabolism Research and Reviews
https://www.readbyqxmd.com/read/29760346/effect-of-sitagliptin-on-coronary-flow-reserve-assessed-by-magnetic-resonance-imaging-in-type-2-diabetic-patients-with-coronary-artery-disease
#15
Keishi Moriwaki, Tetsushiro Takeuchi, Naoki Fujimoto, Toshiki Sawai, Yuichi Sato, Naoto Kumagai, Jun Masuda, Shiro Nakamori, Masaki Ishida, Norikazu Yamada, Mashio Nakamura, Hajime Sakuma, Masaaki Ito, Kaoru Dohi
BACKGROUND: The present study was conducted to assess the cardiovascular effects of dipeptidyl peptidase-4 inhibitors (DPP4i) on coronary flow reserve (CFR), left ventricular (LV) function and endothelial function of the peripheral artery by comparison with those of α-glucosidase inhibitors (αGI) in patients with type 2 diabetes mellitus (T2DM) and coronary artery disease (CAD).Methods and Results:We randomly assigned 30 patients with T2DM and CAD to receive either sitagliptin or voglibose, and 28 patients (age 69±9 years, 75% male, hemoglobin A1c [HbA1c] 6...
May 12, 2018: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/29752167/dipeptidyl-peptidase-4-inhibitor-use-and-risk-of-diabetic-retinopathy-a-population-based-study
#16
N H Kim, J Choi, N H Kim, K M Choi, S H Baik, J Lee, S G Kim
AIMS: This study examined whether dipeptidyl peptidase (DPP)-4 inhibitor use is beneficial or harmful to diabetic retinopathy (DR) compared with other glucose-lowering agents in patients with type 2 diabetes (T2D). METHODS: From a population-based cohort provided by the National Health Insurance Service in Korea, 67,743 adults with T2D were identified as having been treated with oral glucose-lowering agents between 2008 and 2013. Matching (1:1) was performed for two groups comparing ever-use (cases) and never-use (controls) of DPP-4 inhibitors (n=14,522 in each group)...
March 27, 2018: Diabetes & Metabolism
https://www.readbyqxmd.com/read/29751919/effect-of-enzymatic-hydrolysis-on-bioactive-properties-and-allergenicity-of-cricket-gryllodes-sigillatus-protein
#17
Felicia Hall, Philip E Johnson, Andrea Liceaga
Food-derived bioactive peptides have gained attention for their role in preventing chronic diseases. Edible insects are viable sources of bioactive peptides owing to their high protein content and sustainable production. In this study, whole crickets (Gryllodes sigillatus) were alcalase-hydrolyzed to a degree of hydrolysis (DH) ranging from 15 to 85%. Antioxidant activity, angiotensin converting enzyme (ACE), and dipeptidyl peptidase-4 (DPP-IV)- inhibition of the cricket protein hydrolysates (CPH) were evaluated before and after simulated gastrointestinal digestion (SGD)...
October 1, 2018: Food Chemistry
https://www.readbyqxmd.com/read/29749760/plant-dipeptidyl-peptidase-iv-inhibitors-as-antidiabetic-agents-a-brief-review
#18
Gulmira Turdu, Hongwei Gao, Yingying Jiang, Madina Kabas
Diabetes mellitus is an increasing public health problem in the world. Type 2 diabetes is the most common type of diabetes whose complications contribute to its high death rate. It seriously impacts healthcare systems and patients' quality of life. Therefore, effective measures and new treatment strategies are needed to solve this increasingly serious global problem. In recent years, inhibition of dipeptidyl peptidase IV (DPP-IV) has emerged as a new treatment option for Type 2 diabetes. This article reviews various plant DPP-IV inhibitors that showed inhibition toward enzyme as a major target for the management of Type 2 diabetes...
May 11, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29748970/dipeptidyl-peptidase-4-inhibition-prevents-cell-death-via-extrinsic-and-intrinsic-apoptotic-pathways-in-rat-pancreas-with-insulin-resistance
#19
Gulay Nephan, Zeynep Mine Coskun, Sema Bolkent
The study aims to evaluate the effect of saxagliptin, a specific inhibitor of dipeptidyl peptidase-4 enzymes, on body weight gain, lipid profiles, and cell death through apoptosis in rats with insulin resistance (IR). Male adult Sprague-Dawley rats (n = 32) were divided into 4 groups: control (Ctrl), IR, saxagliptin control, and IR treated with saxagliptin(IR + S). Insulin resistance was induced by 10% fructose in the drinking water for 8 weeks. Saxagliptin (10 mg/kg/day) was administrated by oral gavage for 2 weeks...
May 10, 2018: Cell Biochemistry and Function
https://www.readbyqxmd.com/read/29748368/cardiovascular-effects-of-new-oral-glucose-lowering-agents-dpp-4-and-sglt-2-inhibitors
#20
REVIEW
André J Scheen
Cardiovascular disease (CVD) is a major challenge in the management of type 2 diabetes mellitus. Glucose-lowering agents that reduce the risk of major cardiovascular events would be considered a major advance, as recently reported with liraglutide and semaglutide, 2 glucagon-like peptide-1 receptor agonists, and with empagliflozin and canagliflozin, 2 SGLT-2 (sodium-glucose cotransporter type 2) inhibitors, but not with DPP-4 (dipeptidyl peptidase-4) inhibitors. The present review is devoted to CV effects of new oral glucose-lowering agents...
May 11, 2018: Circulation Research
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