17,508 results match your criteria incretin


Mol Pharmacol 2021 Jul 27. Epub 2021 Jul 27.

Imperial College London, United Kingdom

The glucagon-like peptide-1 receptor (GLP-1R) is a class B G protein-coupled receptor and mainstay therapeutic target for the treatment of type 2 diabetes and obesity. Recent reports have highlighted how biased agonism at the GLP-1R affects sustained glucose-stimulated insulin secretion through avoidance of desensitisation and downregulation. A number of GLP-1R agonists (GLP-1RAs) feature a fatty acid moiety to prolong their pharmacokinetics via increased albumin binding, but the potential for these chemical changes to influence GLP-1R function has rarely been investigated beyond potency assessments for cyclic adenosine monophosphate (cAMP). Read More

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Heterogeneity amongst GLP-1 RA cardiovascular outcome trials results: can definition of established cardiovascular disease be the missing link?

Diabetol Metab Syndr 2021 Jul 27;13(1):81. Epub 2021 Jul 27.

Department of Endocrinology, Diabetes and Metabolism, Centro Hospitalar E Universitário S. João, Porto, Portugal.

Atherosclerotic cardiovascular diseases are the leading cause of adverse outcomes in patients with type 2 diabetes, and all new anti-diabetic agents are mandated to undergo cardiovascular outcome trials (CVOTs). Glucagon-like peptide-1 receptor agonists (GLP-1 RA) are incretin mimetics that reduce blood glucose levels with a low associated risk of hypoglycaemia. CVOTs with different GLP-1 RAs yielded different results in terms of major cardiovascular composite outcome (MACE), with some trials showing superiority in the treatment arm, whereas other simply displayed non-inferiority. Read More

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Effects of prebiotics on postprandial GLP-1, GLP-2 and glucose regulation in patients with type 2 diabetes. A randomised, double-blind, placebo-controlled crossover trial.

Diabet Med 2021 Jul 23:e14657. Epub 2021 Jul 23.

Section of Nutrition and Dietetics, Division of Medicine, Department of Clinical Service, Oslo University Hospital, Norway.

Aims: We aimed to investigate the effect of prebiotic inulin-type fructans versus a control supplement on postprandial levels of glucagon-like peptide-1 and -2 (GLP-1 and -2), glucose, and insulin in patients with type 2 diabetes.

Methods: Adult men and women with type 2 diabetes were randomised in a double-blind, placebo-controlled crossover study. The study participants received 16 g/d inulin-type fructans and 16 g/d control supplement (maltodextrin) for six weeks each in two phases separated by a four weeks washout. Read More

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Purification, identification, and molecular mechanism of DPP-IV inhibitory peptides from defatted Antarctic krill powder.

J Food Biochem 2021 Jul 23:e13872. Epub 2021 Jul 23.

College of Food Science and Technology, Shanghai Ocean University, Shanghai, P. R. China.

Dipeptidyl peptidase-IV (DPP-IV) inhibitors can reduce the blood sugar levels of diabetic patients by preventing the rapid decomposition of incretin hormone and prolonging its physiological effects. In this study, DPP-IV inhibitory peptides FAGDDAPR and LAPPRGSL were isolated from defatted Antarctic krill powder (DAKP) protein by the sequential purification of ultrafiltration, gel filtration chromatography, and RP-HPLC, and IC values of the two peptides were 349.70 ± 3. Read More

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The Evolving Story of Incretins (GIP and GLP-1) in Metabolic and Cardiovascular Disease: A Pathophysiological Update.

Diabetes Obes Metab 2021 Jul 26. Epub 2021 Jul 26.

Charité - Universitätsmedizin Berlin, Klinik für Endokrinologie, Stoffwechsel- und Ernährungsmedizin, Berlin, Germany.

The incretin hormones glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) have their main physiological role in augmenting insulin secretion after their nutrient-induced secretion from the gut. A functioning entero-insular (gut-endocrine pancreas) axis is essential for the maintenance of a normal glucose tolerance. This is exemplified by the incretin effect (greater insulin secretory response to oral as compared to "isoglycaemic" intravenous glucose administration due to the secretion and action of incretin hormones). Read More

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[Exendin-4 promotes autophagy to relieve lipid deposition in a NAFLD cell model by activating AKT/mTOR signaling pathway].

Nan Fang Yi Ke Da Xue Xue Bao 2021 Jul;41(7):1073-1078

Department of Endocrinology, Zhujiang Hospital, Southern Medical University, Guangzhou 510280, China.

Objective: To investigate the effect of exendin-4 on lipid deposition in hepatocytes and explore its possible mechanism for treatment of nonalcoholic fatty liver disease (NAFLD).

Methods: Human normal hepatocyte line LO2 and hepatoma cell line HepG2 were treated with palmitic acid (PA) to mimic hepatocyte steatosis or with combined treatments with PA+exendin-4 or PA+exendin-4+3BDO. Lipid deposition and proliferation of the two cell lines following treatment with PA or PA+exendin-4 were detected using Oil Red O staining and CCK8 assay, and the expression of p-mTOR, m-TOR, p-AKT, AKT and autophagy-related proteins LC3-Ⅰ/Ⅱ and p62 were detected with Western blotting; the expression of GLP-1R was detected with both Western blotting and immunofluorescence assay. Read More

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Diabetic Nephropathy: Challenges in Pathogenesis, Diagnosis, and Treatment.

Nur Samsu

Biomed Res Int 2021 8;2021:1497449. Epub 2021 Jul 8.

Division of Nephrology and Hypertension, Department of Internal Medicine, Medical Faculty of Universitas Brawijaya-Saiful Anwar General Hospital, Malang, Indonesia.

Diabetic nephropathy (DN) is the leading cause of end-stage renal disease worldwide. Chronic hyperglycemia and high blood pressure are the main risk factors for the development of DN. In general, screening for microalbuminuria should be performed annually, starting 5 years after diagnosis in type 1 diabetes and at diagnosis and annually thereafter in type 2 diabetes. Read More

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The Role of Positron Emission Tomography in Bariatric Surgery Research: a Review.

Obes Surg 2021 Jul 25. Epub 2021 Jul 25.

Department of Surgery, Yale University School of Medicine, New Haven, CT, USA.

Bariatric surgery, initially understood as restricting or bypassing the amount of food that reaches the stomach to reduce food intake and/or increase malabsorption of food to promote weight loss, is now recognized to also affect incretin signaling in the gut and promote improvements in system-wide metabolism. Positron emission tomography (PET) is an imaging technique whereby patients are injected with picomolar concentrations of radioactive molecules, below the threshold of having physiological effects, to measure spatial distributions of blood flow, metabolism, receptor, and enzyme pharmacology. Recent advances in both whole-body PET imaging and radioligand development will allow for novel research that may help clarify the roles of peripheral and central receptor/enzyme systems in treating obesity with bariatric surgery. Read More

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Polycystic ovary syndrome and infertility: an update.

Int J Adolesc Med Health 2021 Jul 22. Epub 2021 Jul 22.

Regional Research Institute of Unani Medicine, Srinagar, Jammu and Kashmir, India.

Polycystic ovarian syndrome is the most well-known endocrine condition among women of this generation (PCOS). Symptoms of hyperandrogenism, irregular menstrual periods, and insulin resistance are all traits associated with PCOS. In women with PCOS, the chance of having problems including infertility, insulin resistance, and type 2 diabetes increases. Read More

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An Autonomous Cannabinoid System in Islets of Langerhans.

Front Endocrinol (Lausanne) 2021 5;12:699661. Epub 2021 Jul 5.

Laboratory of Clinical Investigation/Diabetes Section, National Institute on Aging, National Institutes of Health, Baltimore, MD, United States.

While endocannabinoids (ECs) and cannabis were primarily studied for their nervous system effects, it is now clear that ECs are also produced in the periphery where they regulate several physiological processes, including energy storage, glucose and lipid metabolism, insulin secretion and synthesis, and hepatocyte function. Within islet of Langerhans there is an autonomous EC system (ECS). Beta (β)-cells contain all the enzymes necessary for EC synthesis and degradation; ECs are generated in response to cellular depolarization; their paracrine influence on β-cells is mostly through the cannabinoid 1 receptor (CBR) that is present on all β-cells; they modulate basal and glucose- and incretin-induced insulin secretion, and β-cell responses to various stressors. Read More

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A method for constructing GLP-1 overexpression intestinal organoids.

Yi Chuan 2021 Jul;43(7):694-703

Shanghai Key Laboratory of Regulatory Biology, School of Life Sciences, East China Normal University, Shanghai 200241, China.

As a potent insulinotrophic hormone, glucagon-like peptide 1 (GLP-1) is mainly secreted by intestinal L cells, which can effectively promote the release of insulin and thus reduce blood glucose. Therefore, GLP-1 and its analogs have a good prospect in the treatment of type 2 diabetes. In this study, we constructed mouse intestinal organoids that overexpress GLP-1 by optimizing the GLP-1 lentivirus infection method. Read More

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Whey protein preload enhances the active GLP-1 response and reduces circulating glucose in women with polycystic ovarian syndrome.

Nutr Res 2021 Jun 24;92:84-98. Epub 2021 Jun 24.

Nutrition and Food Sciences Department, Texas Woman's University, Denton, TX, USA. Electronic address:

Polycystic ovary syndrome (PCOS) increases risk for development of type 2 diabetes. Whey protein ingestion before a carbohydrate load attenuates blood glucose. For our exploratory, case-control study design, we hypothesized that 35 g whey protein isolate (WPI) preloading would increase postprandial incretins and reduce hyperglycemia in women with PCOS. Read More

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Attenuated Postprandial GLP-1 Response in Parkinson's Disease.

Front Neurosci 2021 2;15:660942. Epub 2021 Jul 2.

Division of Digestive Diseases and Nutrition, Department of Internal Medicine, Rush University Medical Center, Chicago, IL, United States.

The incretin hormone glucagon-like peptide 1 (GLP-1) has neuroprotective effects in animal models of Parkinson's disease (PD), and GLP-1 receptor agonists are associated with clinical improvements in human PD patients. GLP-1 is produced and secreted by intestinal L-cells in response to consumption of a meal. Specifically, intestinal microbiota produce short chain fatty acids (SCFA) which, in turn, promote secretion of GLP-1 into the systemic circulation, from which it can enter the brain. Read More

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Managing pasireotide-associated hyperglycemia: a randomized, open-label, Phase IV study.

Pituitary 2021 Jul 18. Epub 2021 Jul 18.

Wroclaw Medical University, Wroclaw, Poland.

Purpose: Pasireotide is an effective treatment for acromegaly and Cushing's disease, although treatment-emergent hyperglycemia can occur. The objective of this study was to assess incretin-based therapy versus insulin for managing pasireotide-associated hyperglycemia uncontrolled by metformin/other permitted oral antidiabetic drugs.

Methods: Multicenter, randomized, open-label, Phase IV study comprising a core phase (≤ 16-week pre-randomization period followed by 16-week randomized treatment period) and optional extension (ClinicalTrials. Read More

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The dawning of dual-acting incretin drugs.

Shimona Starling

Nat Rev Endocrinol 2021 Jul 16. Epub 2021 Jul 16.

Nature Reviews Endocrinology, .

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Peptidomics: A Review of Clinical Applications and Methodologies.

J Proteome Res 2021 Jul 16. Epub 2021 Jul 16.

University of Cambridge Metabolic Research Laboratories, Level 4, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Cambridge CB2 0QQ, U.K.

Improvements in both liquid chromatography (LC) and mass spectrometry (MS) instrumentation have greatly enhanced proteomic and small molecule metabolomic analysis in recent years. Less focus has been on the improved capability to detect and quantify small bioactive peptides, even though the exact sequences of the peptide species produced can have important biological consequences. Endogenous bioactive peptide hormones, for example, are generated by the targeted and regulated cleavage of peptides from their prohormone sequence. Read More

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The effect of melatonin on incretin hormones - results from experimental and randomized clinical studies.

J Clin Endocrinol Metab 2021 Jul 15. Epub 2021 Jul 15.

Steno Diabetes Center Aarhus, Aarhus University Hospital, Aarhus, Denmark.

Context: Glucose homeostasis is under circadian control through both endocrine and intracellular mechanisms with several lines of evidence suggesting that melatonin affects glucose homeostasis.

Objective: To evaluate the acute in-vivo and in-situ effects of melatonin on secretion of the incretin hormones, GLP-1 and GIP, and their impact on β-cell insulin secretion.

Design: A human randomized, double-blinded, placebo-controlled crossover study combined with a confirmatory in-situ study of perfused rat intestines. Read More

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Placental Transfusion, Timing of Plastic Wrap or Bag Placement, and Preterm Neonates.

Am J Perinatol 2021 Jul 12. Epub 2021 Jul 12.

Department of Biostatistics, Indiana University School of Medicine, Indianapolis, Indiana.

Objective:  Compare delivery room practices and outcomes of infants born at less than 32 weeks' gestation or less than 1,500 g who have plastic wrap/bag placement simultaneously during placental transfusion to those receiving plastic wrap/bag placement sequentially following placental transfusion.

Study Design:  Retrospective analysis of data from a multisite quality improvement initiative to refine stabilization procedures pertaining to placental transfusion and thermoregulation using a plastic wrap/bag. Delivery room practices and outcome data in 590 total cases receiving placental transfusion were controlled for propensity score matching and hospital of birth. Read More

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Use of incretin-based drugs and risk of cholangiocarcinoma: Scandinavian cohort study.

Diabetologia 2021 Jul 13. Epub 2021 Jul 13.

Clinical Epidemiology Division, Department of Medicine, Solna, Karolinska Institutet, Stockholm, Sweden.

Aims/hypothesis: Concerns have been raised regarding a potential association of use of the incretin-based drugs dipeptidyl peptidase 4 (DPP4) inhibitors and glucagon-like peptide-1 (GLP-1)-receptor agonists with risk of cholangiocarcinoma. We examined this association in nationwide data from three countries.

Methods: We used data from nationwide registers in Sweden, Denmark and Norway, 2007-2018, to conduct two cohort studies, one for DPP4 inhibitors and one for GLP-1-receptor agonists, to investigate the risk of incident cholangiocarcinoma compared with an active-comparator drug class (sulfonylureas). Read More

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The enteroendocrine-osseous axis in patients with long-term type 1 diabetes mellitus.

Bone 2021 Jul 8;153:116105. Epub 2021 Jul 8.

Department of Pediatric and Adolescent Endocrinology, Pediatric Institute, Jagiellonian University Medical College, Kraków, Poland. Electronic address:

Introduction: The relationship between the gut and skeleton is increasingly recognized as a component of the regulation of carbohydrate metabolism. The aim of our study was to assess the relationship between bone mineral density (BMD), incretin hormones glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1), intestinotrophic peptide glucagon-like peptide-2 (GLP-2) and osteocalcin isoforms in patients with long-term type 1 diabetes (T1D) when compared to healthy controls.

Methods: Eighty two patients with long term T1D, treated in the Department of Metabolic Diseases and 53 healthy controls were recruited to the study. Read More

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Actions of GLP-1 receptor ligands in the gut.

Br J Pharmacol 2021 Jul 7. Epub 2021 Jul 7.

Department of Biomedical Sciences and NovoNordisk Foundation Center for Basic Metabolic Research, Faculty of Health Sciences, University of Copenhagen.

The incretin hormone glucagon-like peptide-1 (GLP-1) is inactivated by the enzyme DPP-4 even before it leaves the gut but seems to act predominantly via activation of intestinal sensory neurons expressing the GLP-1 receptor. Thus activation of vagal afferents is probably responsible for its effects on appetite and food intake, gastrointestinal secretion and motility, and pancreatic endocrine secretion. However, GLP-1 receptors are widely expressed in the gastrointestinal tract, including epithelial cells in the stomach, and the Brunner glands, in endocrine cells of the gut epithelium, and on mucosal lymphocytes. Read More

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Targeting the GPR119/incretin axis: a promising new therapy for metabolic-associated fatty liver disease.

Cell Mol Biol Lett 2021 Jul 7;26(1):32. Epub 2021 Jul 7.

Institute of Liver Diseases, Shuguang Hospital Affiliated To Shanghai, University of Traditional Chinese Medicine, 528, Zhangheng Road, Shanghai, China.

In the past decade, G protein-coupled receptors have emerged as drug targets, and their physiological and pathological effects have been extensively studied. Among these receptors, GPR119 is expressed in multiple organs, including the liver. It can be activated by a variety of endogenous and exogenous ligands. Read More

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Type 2 Diabetes Medication and Cardiovascular Benefits.

S D Med 2021 Mar;74(3):132-135

Avera Mckennan Hospital and University Center, Sioux Falls, South Dakota.

Diabetes mellitus remains one of the most common and disabling diseases in the world. Patients with diabetes tend to have more cardiovascular complications, regardless of their prior cardiac history. Tight glycemic control has been shown to prevent microvascular complications as it relates to nephropathy and retinopathy; however, it hasn't been proven beneficial in patients with macrovascular diseases, i. Read More

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Indian Expert Review on Use of Teneligliptin in patients with Diabetes and its Safety and Efficacy (INTENSE).

J Assoc Physicians India 2021 Jan;69(1):61-70

Senior Consultant, Apollo Hospitals, Bhubaneswar, Orissa.

Introduction: Management of diabetes in India remains less than satisfactory despite a huge prevalence of type 2 diabetes (T2D). Associated obesity, inadequate lifestyle modifications and burden of treatment costs are certain major issues contributing to inadequate management of diabetes in India.

Aim: To evaluate the use of Teneligliptin in patients with diabetes and its safety, efficacy and cost effectiveness especially in Indian patients with T2D. Read More

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January 2021

The Postprandial Glycaemic and Hormonal Responses Following the Ingestion of a Novel, Ready-to-Drink Shot Containing a Low Dose of Whey Protein in Centrally Obese and Lean Adult Males: A Randomised Controlled Trial.

Front Endocrinol (Lausanne) 2021 18;12:696977. Epub 2021 Jun 18.

Population Health Sciences Institute, Newcastle University, Newcastle upon Tyne, United Kingdom.

Purpose: Elevated postprandial glycaemia [PPG] increases the risk of cardiometabolic complications in insulin-resistant, centrally obese individuals. Therefore, strategies that improve PPG are of importance for this population. Consuming large doses of whey protein [WP] before meals reduces PPG by delaying gastric emptying and stimulating the secretion of the incretin peptides, glucose-dependent insulinotropic polypeptide [GIP] and glucagon-like peptide 1 [GLP-1]. Read More

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Anti-diabetic drugs and NASH: from current options to promising perspectives.

Expert Opin Investig Drugs 2021 Jul 12:1-13. Epub 2021 Jul 12.

Department of Endocrinology, Université De Nantes, CHU Nantes, CNRS, INSERM, L'institut Du Thorax, Nantes, France.

: Accumulating evidence supports a bidirectional association between nonalcoholic steatohepatitis (NASH) and type 2 diabetes (T2D). There is a clinical challenge to consider pharmaceutical strategies targeting the metabolic dysfunction common to NASH and T2D pathogenesis.: By using PubMed, we performed a literature search to review the potential beneficial effect of anti-diabetic and metabolic investigational drugs on NASH. Read More

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Breast Cancer, Diabetes Mellitus and Glucagon-Like Peptide-1 Receptor Toward Exploring Their Possible Associations.

Breast Cancer Res Treat 2021 Aug 2;189(1):39-48. Epub 2021 Jul 2.

Department of Pathology, Tohoku University Graduate School of Medicine, 2-1 Seiryo-machi, Aoba-ku, Sendai, Miyagi, 980-8575, Japan.

Purpose: Diabetes Mellitus (DM) has been one of the well known risk factors of breast cancer (BC) development and also associated with adverse clinical outcomes of BC patients. Glucagon-like peptide-1 (GLP-1) receptor agonists have been used as antidiabetic therapeutic agents and recent epidemiological studies have reported their use to be correlated with increased BC risks. However, biological or pathological details have remained unknown. Read More

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Sex differences in oxidative stress level and antioxidative enzymes expression and activity in obese pre-diabetic elderly rats treated with metformin or liraglutide.

Croat Med J 2021 Jun;62(3):215-226

Ines Drenjančević, Institute and Department of Physiology and Immunology, Faculty of Medicine University Josip Juraj Strossmayer of Osijek, J. Huttlera 4, 31 000 Osijek, Croatia,

Aim: To determine the effects of metformin or liraglutide on oxidative stress level and antioxidative enzymes gene expression and activity in the blood and vessels of pre-diabetic obese elderly Sprague-Dawley (SD) rats of both sexes.

Methods: Male and female SD rats were assigned to the following groups: a) control group (fed with standard rodent chow); b) high-fat and high-carbohydrate diet (HSHFD) group fed with HSHFD from 20-65 weeks of age; c) HSHFD+metformin treatment (50 mg/kg/d s.c. Read More

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A 2021 Update on the Use of Liraglutide in the Modern Treatment of 'Diabesity': A Narrative Review.

Medicina (Kaunas) 2021 Jun 29;57(7). Epub 2021 Jun 29.

Department ME2, Faculty of Medicine, "George Emil Palade" University of Medicine, Pharmacy, Science and Technology, 540136 Targu Mures, Romania.

Obesity and type 2 diabetes mellitus have become a significant public health problem in the past decades. Their prevalence is increasing worldwide each year, greatly impacting the economic and personal aspects, mainly because they frequently coexist, where the term "diabesity" may be used. The drug class of glucagon-like peptide 1 receptor agonists (GLP-1 RAs) is one of the most modern therapy options in managing these metabolic disorders. Read More

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Dipeptidyl Peptidase (DPP)-IV Inhibitors with Antioxidant Potential Isolated from Natural Sources: A Novel Approach for the Management of Diabetes.

Pharmaceuticals (Basel) 2021 Jun 18;14(6). Epub 2021 Jun 18.

Department of Medical Biotechnology, Yeungnam University, Gyeongsan 38541, Korea.

Type 2 diabetes mellitus (T2DM) is characterized by hyperglycemia that is predominantly caused by insulin resistance or impaired insulin secretion, along with disturbances in carbohydrate, fat and protein metabolism. Various therapeutic approaches have been used to treat diabetes, including improvement of insulin sensitivity, inhibition of gluconeogenesis, and decreasing glucose absorption from the intestines. Recently, a novel approach has emerged using dipeptidyl peptidase-IV (DPP-IV) inhibitors as a possible agent for the treatment of T2DM without producing any side effects, such as hypoglycemia and exhaustion of pancreatic β-cells. Read More

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