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Gliptins

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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
#1
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/29748368/cardiovascular-effects-of-new-oral-glucose-lowering-agents-dpp-4-and-sglt-2-inhibitors
#2
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
https://www.readbyqxmd.com/read/29698678/citrus-bioflavonoids-possess-dipeptidyl-peptidase-4-inhibition-activity-similar-to-gliptin-antidiabetic-medication
#3
Ankit Gupta, Glenn A Jacobson, John R Burgess, Herbert F Jelinek, David S Nichols, Christian K Narkowicz, Hayder A Al-Aubaidy
This study demonstrates the Dipeptidyl peprtidase-4 (DPP-4) inhibition activity of citrus bioflavonoid nutraceuticals as compared to known gliptins. Citrus bioflavonoid standards and three commercially available citrus bioflavonoid supplements (Thompson's Super Bioflavonoid Complex® (SB), Ethical Nutrient Citrus Plus Vitamin C® (EN), and Country Life Citrus Bioflavonoid & Rutin® (CB)) were considered in this study. Ultra-performance liquid chromatography-mass spectrometry (UPLC-MS) analysis was undertaken to identify the citrus bioflavonoids present in each supplement and the DPP-4 inhibitory activity was determined using the DPP-4 fluorometric assay...
April 23, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29667232/the-pleiotropic-cardiovascular-effects-of-dipeptidyl-peptidase-4-inhibitors
#4
REVIEW
Angelo Avogaro, Gian Paolo Fadini
Patients with Type 2 Diabetes have an excess risk for cardiovascular disease. One of the several approaches, included in the Guidelines for the management of Type 2 Diabetes, is based on dipeptidyl peptidase 4 (DPP-4; also termed CD26) inhibitors (DPP-4-I), also called gliptins. Gliptins inhibit the degradation of glucagon-like peptide-1 GLP-1RA: this effect is associated with increased circulating insulin-to-glucagon ratio, and a consequent reduction of HbA1c. Beside incretin hormones, there are several proteins that may be affected by DPP-4 and its inhibition: among these some are relevant for the cardiovascular system homeostasis such as SDF-1α and its receptor CXCR4, brain natriuretic peptides, neuropeptide Y, and peptide YY...
April 17, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29619987/comorbidities-of-bullous-pemphigoid-in-a-finnish-cohort
#5
Anna Pankakoski, Harri Sintonen, Annamari Ranki, Nicolas Kluger
The incidence of bullous pemphigoid (BP) is increasing in Finland. To investigate the clinical presentation, comorbidities, and medications in a cohort of Finnish patients with confirmed BP managed in a university hospital setting. An observational retrospective study of all consecutive patients diagnosed with BP in 2012-2013 at the Department of dermatology, HUCH. The prevalence of the most common comorbidities was compared to that in a sample population aged over 30 years. Seventy patients were included (mean age: 77 years at diagnosis)...
April 5, 2018: European Journal of Dermatology: EJD
https://www.readbyqxmd.com/read/29580624/antidiabetic-gliptins-affect-biofilm-formation-by-streptococcus-mutans
#6
Arpan De, Arianna Pompilio, Jenifer Francis, Iain C Sutcliffe, Gary W Black, Giulio Lupidi, Dezemona Petrelli, Luca A Vitali
Streptococcus mutans, a dental caries causing odontopathogen, produces X-prolyl dipeptidyl peptidase (Sm-XPDAP, encoded by pepX), a serine protease known to have a nutritional role. Considering the potential of proteases as therapeutic targets in pathogens, this study was primarily aimed at investigating the role of Sm-XPDAP in contributing to virulence-related traits. Dipeptidyl peptidase (DPP IV), an XPDAP analogous enzyme found in mammalian tissues,is a well known therapeutic target in Type II diabetes. Based on the hypothesis that gliptins, commonly used as anti-human-DPP IV drugs, may affect bacterial growth upon inhibition of Sm-XPDAP, we have determined their ex vivo antimicrobial and anti-biofilm activity towards S...
April 2018: Microbiological Research
https://www.readbyqxmd.com/read/29569760/changing-prevalence-of-diabetes-mellitus-in-bullous-pemphigoid-it-is-the-dipeptidyl-peptidase-4-inhibitors
#7
A Gravani, G Gaitanis, T Tsironi, S Tigas, I D Bassukas
We read with interest the letter by Fania et al1 on the increased prevalence of diabetes mellitus type 2 (DM2) among patients diagnosed with bullous pemphigoid (BP) after 2007. Employing a retrospective study design the authors demonstrate an abrupt raise in the prevalence of DM2 among BP patients in relation to those with pemphigus. They conclude that this trend might stem from an increase in DM2 comorbidity among BP patients. Furthermore, the recorded accumulation of BP cases is attributed to the intake of dipeptydil peptidase-4 inhibitors (DPP-4, gliptins)...
March 23, 2018: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/29531541/sitagliptin-accelerates-endothelial-regeneration-after-vascular-injury-independent-from-glp1-receptor-signaling
#8
Friederike Remm, Nicolle Kränkel, Daniela Lener, Daniel J Drucker, Sieghart Sopper, Christoph Brenner
Introduction: DPP4 inhibitors (gliptins) are commonly used antidiabetic drugs for the treatment of type 2 diabetes. Gliptins also act in a glucose-independent manner and show vasoregenerative effects. We have shown that gliptins can remarkably accelerate vascular healing after vascular injury. However, the underlying mechanisms remain unclear. Here, we examined potential signaling pathways linking gliptins to enhanced endothelial regeneration. Methods and Results: We used wild-type and GLP1 receptor knockout ( Glp1r -/- ) mice to investigate the underlying mechanisms of gliptin-induced reendothelialization...
2018: Stem Cells International
https://www.readbyqxmd.com/read/29521244/synthesis-structural-characterization-and-docking-studies-of-sulfamoyl-phenyl-acid-esters-as-dpp-iv-inhibitors
#9
Reema Abdelkareem Abu Khalaf, Dima Sabbah, Eveen Al-Shalabi, Iyad Al-Sheikh, Ghadeer Albadawi, Ghassan Abu Sheikha
BACKGROUND: Diabetes mellitus is a major worldwide health concern that has several serious complications including retinopathy, neuropathy, nephropathy and macrovascular diseases. OBJECTIVE: Dipeptidyl peptidase-IV (DPP-IV) inhibitors, gliptins, are a new class of antidiabetic agents that potentiates the action of incretins in decreasing the blood glucose levels. METHODS: In the present study, synthesis and characterization of a series of ten N4-sulfonamido-acrylic and phthalamic acid methyl esters (3a-e and 5a-e) were achieved...
March 8, 2018: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/29468916/the-safety-of-gliptins-updated-data-in-2018
#10
REVIEW
André Jacques Scheen
Dipeptidyl peptidase-4 inhibitors (DPP-4is) are generally considered as glucose-lowering agents with a safe profile in type 2 diabetes. Areas covered: An updated review of recent safety data from randomised controlled trials, observational studies, meta-analyses, pharmacovigilance reports regarding alogliptin, linagliptin, saxagliptin, sitagliptin, and vildagliptin, with a special focus on risks of hypoglycemia, pancreatitis and pancreatic cancer, major cardiovascular events, hospitalisation for heart failure and other new safety issues, such as bone fractures and arthralgia...
April 2018: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/29285456/gemigliptin-newer-promising-gliptin-for-type-2-diabetes-mellitus
#11
REVIEW
Manish Gutch, Abhay Joshi, Sukriti Kumar, Avinash Agarwal, Rajendra Kumar Pahan, Syed Mohd Razi
The dipeptidyl peptidase-4 (DPP-4) inhibitors have facilitated the management of type 2 diabetes mellitus (T2DM) owing to their superior efficacy and safety with low incidence of adverse effects. Gemigliptin is a new member of this family of drugs, and studies have revealed certain advantages of gemigliptin use compared to its previous congeners. Besides, this drug has also been studied for the treatment of T2DM as monotherapy, in combination with metformin or other oral antidiabetic drugs and in T2DM with moderate-to-severe renal failure...
November 2017: Indian Journal of Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29127747/-treatment-strategy-of-type-2%C3%A2-diabetes-used-in-czech-republic-after-metformin-therapy-failure
#12
Štěpán Svačina, Petra Ovesná, Matyáš Kuhn, Martina Nováčková
INTRODUCTION: Type 2 diabetes is an enormous medical problem caused by increasing prevalence of the disease and increasing prevalence of severe chronic complications of diabetes. New ADA/EASD guidelines and also Czech diabetes society guidelines enable effective individual approach to the patient. Goal of the therapy is optimal compensation of diabetes and prevention of acute and chronic complications of diabetes and decrease of mortality. Diabetes therapy is started by education in diet a regime combined with metformin...
2017: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29058840/-use-of-oral-glucose-lowering-agents-in-patients-with-renal-impairment
#13
A J Scheen, N Paquot
Patients with type 2 diabetes (T2D) and chronic kidney disease (CKD) are increasingly numerous, especially in the elderly population. Surprisingly, this situation is often under-recognized or even neglected in clinical practice. Yet, most oral antidiabetic (OAD) agents have limitations in case of renal impairment, either because they require a dose reduction, or are contra-indicated mainly for safety reasons. This clinical case gives the opportunity to discuss the modalities of prescription and cautions to be taken when using most commonly prescribed OAD, metformin, insulin secretagogues (sulfonylureas, repaglinide), DPP-4 inhibitors (gliptins) and SGLT2 inhibitors, in a patient with T2D and CKD...
October 2017: Revue Médicale de Liège
https://www.readbyqxmd.com/read/29031704/evaluation-of-cooperative-antileukemic-effects-of-nilotinib-and-vildagliptin-in-ph-chronic-myeloid-leukemia
#14
Michael Willmann, Irina Sadovnik, Gregor Eisenwort, Martin Entner, Tina Bernthaler, Gabriele Stefanzl, Emir Hadzijusufovic, Daniela Berger, Harald Herrmann, Gregor Hoermann, Peter Valent, Thomas Rülicke
Chronic myeloid leukemia (CML) is a stem cell (SC) neoplasm characterized by the BCR/ABL1 oncogene. Although the disease can be kept under control using BCR/ABL1 tyrosine kinase inhibitors (TKIs) in most cases, some patients relapse or have resistant disease, so there is a need to identify new therapeutic targets in this malignancy. Recent data suggest that leukemic SCs (LSCs) in CML display the stem-cell (SC)-mobilizing cell surface enzyme dipeptidyl-peptidase IV (DPPIV = CD26) in an aberrant manner. In the present study, we analyzed the effects of the DPPIV blocker vildagliptin as single agent or in combination with the BCR/ABL1 TKI imatinib or nilotinib on growth and survival of CML LSCs in vitro and on LSC engraftment in an in vivo xenotransplantation nonobese diabetic SCID-IL-2Rγ-/- (NSG) mouse model...
January 2018: Experimental Hematology
https://www.readbyqxmd.com/read/28932239/computational-analysis-of-gynura-bicolor-bioactive-compounds-as-dipeptidyl-peptidase-iv-inhibitor
#15
Lina Rozano, Muhammad Redha Abdullah Zawawi, Muhamad Aizuddin Ahmad, Indu Bala Jaganath
The inhibition of dipeptidyl peptidase-IV (DPPIV) is a popular route for the treatment of type-2 diabetes. Commercially available gliptin-based drugs such as sitagliptin, anagliptin, linagliptin, saxagliptin, and alogliptin were specifically developed as DPPIV inhibitors for diabetic patients. The use of Gynura bicolor in treating diabetes had been reported in various in vitro experiments. However, an understanding of the inhibitory actions of G. bicolor bioactive compounds on DPPIV is still lacking and this may provide crucial information for the development of more potent and natural sources of DPPIV inhibitors...
2017: Advances in Bioinformatics
https://www.readbyqxmd.com/read/28879786/pharmacological-management-of-type-2-diabetes-what-s-new-in-2017
#16
REVIEW
André J Scheen
Novelties in the management of type 2 diabetes are dominated by the commercialisation of new glucose-lowering agents, which offer alternatives to older antidiabetic medications, and by the publication of several prospective placebo-controlled outcome trials, which demonstrated not only cardiovascular safety but also cardiovascular and renal protection with some new medications. Areas covered: Updates regarding the use of glucose-lowering agents are discussed from a clinical point of view. Some new viewpoints concern older antidiabetic agents such as metformin, sulfonylureas and glitazones whose benefit-risk balance has been revisited, especially in high risk patients...
December 2017: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/28837278/-therapeutic-options-for-a-type-2-diabetic-patient-not-well-controlled-with-metformin-plus-basal-insulin
#17
André J Scheen, Nicolas Paquot
In a patient with type 2 diabetes not well controlled with a basal insulin - metformin combination, several therapeutic options may be considered: intensifying insulin therapy with different schemes (appropriate titration using a more favourable basal insulin analogue, adding one, two or three rapid-acting insulin analogues, shift to two or three premix insulin injections), adding a dipeptidyl peptidase-4 inhibitor (gliptin) or an inhibitor of sodium-glucose cotransporters type 2 (gliflozin), or combining a glucagon-like peptide-1 receptor agonist with basal insulin...
August 23, 2017: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28837277/-dpp-4-or-sglt2-inhibitor-added-to-metformin-alone-in-type-2-diabetes
#18
Nicolas Paquot, André J Scheen
After failure of a monotherapy with metformin, dipeptidyl peptidase-4 inhibitors (gliptins) and sodium-glucose cotransporters type 2 (gliflozins) offer an alternative to the add-on of a sulphonylurea, especially in diabetic patients at risk of hypoglycaemia. The choice between a gliptin and a gliflozin may be guided by the individual patient characteristics : rather a gliptin in a patient without obesity or severe hyperglycaemia, in an elderly patient, with a frailty profile or with renal impairment; rather a gliflozin in an obese patient, with hypertension, hyperuricaemia, antecedents of cardiovascular disease (especially heart failure), without advanced renal insufficiency and with a low risk of urinary/genital infections or events linked to dehydration such as hypotension...
August 23, 2017: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28815568/gliptin-therapy-reduces-hepatic-and-myocardial-fat-in-type-2-diabetic-patients
#19
Lana Kosi-Trebotic, Anita Thomas, Jürgen Harreiter, Marek Chmelik, Siegfried Trattnig, Alexandra Kautzky-Willer
BACKGROUND: Increased hepatic fat and cardiac fat are common in patients with type 2 diabetes mellitus (T2DM) and are associated with a greater risk of liver fibrosis and cardiovascular (CV) events. Sex-specific differences of dipeptidyl peptidase-four (DPP-4) inhibitor effects on hepatic (HCL) and myocardial fat content (MYCL) have not yet been evaluated. METHOD: Forty-one T2DM patients (20 male, 21 female) received a gliptin add-on therapy if HbA1c goals were not reached under metformin monotherapy...
August 16, 2017: European Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28701284/cost-effectiveness-analysis-of-different-dipeptidyl-peptidase-4-inhibitor-drugs-for-treatment-of-type-2-diabetes-mellitus
#20
Maurílio de Souza Cazarim, Estael Luzia Coelho da Cruz-Cazarim, André de Oliveira Baldoni, Thais Bueno Enes Dos Santos, Paula Gonçalves de Souza, Ingrid de Almeida Silva, Roberta Niriam Reis Rodrigues, Alda Cristina Franco Correa Maia, Leonardo Régis Leira Pereira, Cristina Sanches
INTRODUCTION: Type 2 diabetes mellitus (T2DM) has burdened health systems in the world to the value of 500 billion dollars/year. Dipeptidyl peptidase 4 inhibitors (DPP-4 Inhibitors) have been strongly associated with spending on the treatment of T2DM by the courts in Brazil. The aim of this study was to estimate the most cost-effective DPP-4 Inhibitor for T2DM treatment. A pharmacoeconomic study of cost-effectiveness was performed in a medium-sized municipality in Minas Gerais state, Brazil...
July 3, 2017: Diabetes & Metabolic Syndrome
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