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Exendin-4

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https://www.readbyqxmd.com/read/29462693/two-novel-dual-glp-1-gip-receptor-agonists-are-neuroprotective-in-the-mptp-mouse-model-of-parkinson-s-disease
#1
Peng Feng, Xiangjian Zhang, Dongfang Li, Chenhui Ji, Ziyue Yuan, Ruifang Wang, Guofang Xue, Guanglai Li, Christian Hölscher
Type 2 diabetes mellitus (T2DM) is a risk factors for developing Parkinson's disease (PD). Insulin desensitization is observed in the brains of PD patients, which may be an underlying mechanism that promotes neurodegeneration. Incretin hormones are growth factors that can re-sensitize insulin signalling. We have previously shown that analogues of the incretins GLP-1 or GIP have neuroprotective effects in the MPTP mouse model of PD. Novel dual GLP-1/GIP receptor agonists have been developed as treatments for T2DM...
February 17, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29430842/glucagon-like-peptide-1-glp-1-based-therapeutics-current-status-and-future-opportunities-beyond-type-2-diabetes
#2
Jia Ying Cheang, Peter Michael Moyle
Glucagon-like peptide-1 (GLP-1) is secreted by intestinal L-cells following food intake, and plays an important role in glucose homeostasis due to its stimulation of glucose-dependent insulin secretion. Further, GLP-1 is also associated with protective effects on pancreatic β-cells and the cardiovascular system, reduced appetite, and weight loss, making GLP-1 derivatives an exciting treatment for type 2 diabetes and obesity. Despite these benefits, wild-type GLP-1 exhibits a short circulation time, due to its poor metabolic stability and rapid renal clearance, and needs to be administered by injection, making it a poor therapeutic agent...
February 11, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29423016/exendin-4-promotes-the-osteogenic-differentiation-of-osteoblasts-via-the-hedgehog-gli1-signaling-pathway
#3
Liu Gao, Shilun Li, Yukun Li
This study aimed to investigate the effect and mechanisms of Exendin-4 mediated-Hedgehog/Gli1 signaling pathway on the differentiation of osteoblasts in mouse. The alkaline phosphate activity, alizarin red staining and expression of Gli1, GLP-1R, Hedgehog, Runx2 and osteocalcin were analyzed using PCR and Western blot analysis after treating the osteoblastic cell line MC3T3-E1 with Exendin-4. Osteoblasts were treated with Gli1-siRNA and Hedgehog receptor antagonist Cyclopamine (Cy) and analyzed for their impact on the Hedgehog/Gli1 signaling pathway...
2018: American Journal of Translational Research
https://www.readbyqxmd.com/read/29421245/effect-of-glucagon-like-peptide-1-analogue-exendin-4-on-cognitive-functions-in-type-2-diabetes-mellitus-possible-modulation-of-brain-derived-neurotrophic-factor-and-brain-visfatin
#4
O M Abdelwahed, O M Tork, M M Gamal El Din, L Rashed, M Zickri
BACKGROUND: Brain derived neurotrophic factor (BDNF) is one of the most essential neurotrophic factors in the brain. BDNF is involved in learning, memory and locomotion suggesting it as a target in type 2 diabetes mellitus (T2DM) associated cognitive changes. Visfatin; an adipokine discovered to be expressed in the brain; was found to have multiple effects including its participation in keeping energy supply to the cell and is consequentially involved in cell survival. Its role in cognitive functions in T2DM was not studied before...
February 5, 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29414148/exenatide-modulates-metalloproteinase-expression-in-human-cardiac-smooth-muscle-cells-via-the-inhibition-of-akt-signaling-pathway
#5
Enrique Gallego-Colon, Agnieszka Klych-Ratuszny, Agnieszka Kosowska, Wojciech Garczorz, Mohammad Reza F Aghdam, Michal Wozniak, Tomasz Francuz
BACKGROUND: Incretin analogue drugs, a FDA-approved treatment in diabetes, has been tested for its therapeutic properties as modulators of atherosclerosis. We investigated the effects of incretin drugs on the modulation of gene expression and protein levels of matrix metalloproteinases (MMPs) as well as their inhibitors - tissue inhibitors of metalloproteinases (TIMPs) in coronary artery smooth muscle cells (hCASMC) in the context of atherosclerotic plaque formation and inflammation. METHODS: TNFα-stimulated hCASMC were treated with Glucagon-like Peptide 1 (GLP-1) (10 nM and 100 nM) and Exendin-4 (1 nM and 10 nM)...
October 4, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29412820/a-novel-glp-1-xenin-hybrid-peptide-improves-glucose-homeostasis-circulating-lipids-and-restores-gip-sensitivity-in-high-fat-fed-mice
#6
Annie Hasib, Ming T Ng, Dawood Khan, Victor A Gault, Peter R Flatt, Nigel Irwin
Combined modulation of peptide hormone receptors including, glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP) and xenin, have established benefits for the treatment of diabetes. The present study has assessed the biological actions and therapeutic efficacy of a novel exendin-4/xenin-8-Gln hybrid peptide, both alone and in combination with the GIP receptor agonist (DAla2)GIP. Exendin-4/xenin-8-Gln was enzymatically stable and exhibited enhanced insulin secretory actions when compared to its parent peptides...
February 2018: Peptides
https://www.readbyqxmd.com/read/29412813/insulin-and-igf-1-receptor-autocrine-loops-are-not-required-for-exendin-4-induced-changes-to-pancreatic-%C3%AE-cell-bioenergetic-parameters-and-metabolism-in-brin-bd11-cells
#7
Jordan Rowlands, Vinicius Cruzat, Rodrigo Carlessi, Philip Newsholme
Pharmacological long lasting Glucagon-like peptide-1 (GLP-1) analogues, such as Exendin-4, have become widely used diabetes therapies. Chronic GLP-1R stimulation has been linked to β-cell protection and these pro-survival actions of GLP-1 are dependent on the activation of the mammalian target of rapamycin (mTOR) leading to accumulation of Hypoxia inducible factor 1 alpha (HIF-1α). Recent studies from our lab indicate that prolonged GLP-1R stimulation promotes metabolic reprograming of β-cells towards a highly glycolytic phenotype and activation of the mTOR/HIF-1α pathway was required for this action...
February 2018: Peptides
https://www.readbyqxmd.com/read/29406832/coagonist-of-glp-1-and-glucagon-receptors-ameliorates-non-alcoholic-fatty-liver-disease
#8
Vishal J Patel, Amit Arvind Joharapurkar, Samadhan Kshirsagar, Maulik S Patel, Brijesh K Sutariya, Hiren M Patel, Dheerendra Pandey, Dipam Patel, Ramchandra Ranvir, Shekhar Kadam, Rajesh Bahekar, Mukul Jain
Nonalcoholic fatty liver disease (NAFLD) is often associated with obesity and type 2 diabetes. Coagonist of glucagon-like peptide-1 receptor (GLP-1R) and glucagon receptor (GCGR) are under clinical investigation for the treatment of obesity and type 2 diabetes. In this study, we have demonstrated the effect of a balanced coagonist in the treatment of NAFLD using mice models. GLP-1R agonist exendin-4, glucagon, and coagonist (Aib2 C24 Chimera2) were administered to C57BL6/J mice, in which NAFLD was induced by carbon tetrachloride (CCl4) treatment after in high fat diet (HFD) feeding, and CDAHFD (choline-deficient, L-amino acid-defined, HFD)...
February 6, 2018: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/29404215/equine-glucagon-like-peptide-1-receptor-physiology
#9
Murad H Kheder, Simon R Bailey, Kevin J Dudley, Martin N Sillence, Melody A de Laat
Background: Equine metabolic syndrome (EMS) is associated with insulin dysregulation, which often manifests as post-prandial hyperinsulinemia. Circulating concentrations of the incretin hormone, glucagon-like peptide-1 (GLP-1) correlate with an increased insulin response to carbohydrate intake in animals with EMS. However, little is known about the equine GLP-1 receptor (eGLP-1R), or whether GLP-1 concentrations can be manipulated. The objectives were to determine (1) the tissue localisation of the eGLP-1R, (2) the GLP-1 secretory capacity of equine intestine in response to glucose and (3) whether GLP-1 stimulated insulin secretion from isolated pancreatic islets can be attenuated...
2018: PeerJ
https://www.readbyqxmd.com/read/29399966/morphologically-invisible-proinsulin-secreting-adenoma-detected-by-ga-68-exendin-4-glp-1-receptor-positron-emission-tomography-ct
#10
Christoph Werner, Amelie Lupp, Robert Drescher, Martin Freesmeyer, Masoud Mireskandari, Christian Stoykow, Astrid Bauschke, Ulrich A Müller
This case report of a young man suffering from recurring hypoglycaemia illustrates a rare condition of a neuroendocrine tumour, predominantly secreting proinsulin and invisible to conventional imaging approaches. Only a GLP-1 receptor PET/CT using Exendin-4 visualized the pancreatic lesion and enabled curative therapy, confirming the diagnostic value of this tracer for detection of neuroendocrine tumours. As only few publications on this topic are available, an overview of the available data is also given. The known cut-off value of 60% for proinsulin level indicating malignancy is critically discussed...
February 5, 2018: Journal of Medical Imaging and Radiation Oncology
https://www.readbyqxmd.com/read/29372538/sustained-exenatide-delivery-via-intracapsular-microspheres-for-improved-survival-and-function-of-microencapsulated-porcine-islets
#11
Benjamin Lew, In-Yong Kim, Hyungsoo Choi, Kyekyoon Kevin Kim
The ability of glucagon-like peptide-1 analogs to enhance glucose-dependent insulin secretion and to inhibit β cell apoptosis could be of potential benefit for islet transplantation. In this study, we investigated the effect of sustained local delivery of exenatide, a synthetic exendin-4, on the in vitro viability and function of encapsulated porcine islets. Prior to encapsulation, we fabricated exenatide-loaded poly(latic-co-glycolic acid) microspheres, and investigated their release behavior with different initial drug-loading amounts...
January 25, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29366148/positron-emission-tomography-tracer-68ga-nodaga-exendin-4-detects-glucagon-like-peptide-1-receptor-expression-in-mouse-atherosclerotic-vascular-lesions
#12
Mia Ståhle, Sanna Hellberg, Jenni Virta, Heidi Liljenbäck, Olli Metsälä, Matti Jauhiainen, Pekka Saukko, Seppo Ylä-Herttuala, Pirjo Nuutila, Juhani Knuuti, Antti Saraste, Anne Roivainen
No abstract text is available yet for this article.
August 2017: Atherosclerosis
https://www.readbyqxmd.com/read/29351476/human-endoc-%C3%AE-h1-%C3%AE-cells-form-pseudoislets-with-improved-glucose-sensitivity-and-enhanced-glp-1-signaling-in-the-presence-of-islet-derived-endothelial-cells
#13
Michael G Spelios, Lauren A Afinowicz, Regine C Tipon, Eitan M Akirav
Three-dimensional (3D) pseudoislets (PIs) can be used for the study of insulin-producing β-cells in free-floating islet-like structures similar to that of primary islets. Previously, we demonstrated the ability of islet-derived endothelial cells (iECs) to induce PIs using murine insulinomas, where PI formation enhanced insulin production and glucose responsiveness. In this report, we examined the ability of iECs to spontaneously induce the formation of free-floating 3D PIs using the EndoC-βH1 human β-cell line murine MS1 iEC line...
January 16, 2018: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29348573/exendin-4-encapsulated-dissolving-microneedle-arrays-for-efficient-treatment-of-type-2-diabetes
#14
Shayan Fakhraei Lahiji, Yoojung Jang, Inyoung Huh, Huisuk Yang, Mingyu Jang, Hyungil Jung
Dissolving microneedles (DMNs) are microscopic needles capable of delivering encapsulated compounds and releasing them into the skin in a minimally invasive manner. Most studies indicate that encapsulating therapeutics in DMNs is an efficacious approach; however, the importance of evaluating the activity of encapsulated compounds, during the fabrication process, has not been examined in detail. Conducting an analysis of thermal, chemical, and physical stress factors, including temperature, pH, and the interaction of the polymer and therapeutics mixture during preparation, is essential for retaining the activity of encapsulated therapeutics during and after fabrication...
January 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29335487/increased-expression-of-glp-1r-in-proliferating-islets-of-men1-mice-is-detectable-by-68ga-ga-do3a-vs-cys40-exendin-4-pet
#15
Azita Monazzam, Joey Lau, Irina Velikyan, Su-Chen Li, Masoud Razmara, Ulrika Rosenström, Olof Eriksson, Britt Skogseid
Multiple endocrine neoplasia type 1 (MEN1) is an endocrine tumor syndrome caused by heterozygous mutations in the MEN1 tumor suppressor gene. The MEN1 pancreas of the adolescent gene carrier frequently contain diffusely spread pre-neoplasias and microadenomas, progressing to macroscopic and potentially malignant pancreatic neuroendocrine tumors (P-NET), which represents the major death cause in MEN1. The unveiling of the molecular mechanism of P-NET which is not currently understood fully to allow the optimization of diagnostics and treatment...
January 15, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29327400/a-vitamin-b12-conjugate-of-exendin-4-improves-glucose-tolerance-without-associated-nausea-or-hypophagia-in-rodents
#16
Elizabeth G Mietlicki-Baase, Claudia G Liberini, Jayme L Workinger, Ron L Bonaccorso, Tito Borner, David J Reiner, Kieran Koch-Laskowski, Lauren E McGrath, Rinzin Lhamo, Lauren M Stein, Bart C De Jonghe, George G Holz, Christian L Roth, Robert P Doyle, Matthew R Hayes
AIMS: While pharmacological glucagon-like peptide-1 receptor (GLP-1R) agonists are FDA-approved for treating type 2 diabetes mellitus (T2DM) and obesity, a major side effect is nausea/malaise. We recently developed a conjugate of vitamin B12 bound to the GLP-1R agonist exendin-4 (Ex4), which displays enhanced proteolytic stability and retention of GLP-1R agonism. Here, we evaluate whether the conjugate (B12-Ex4) can improve glucose tolerance without producing anorexia and malaise. MATERIALS AND METHODS: We evaluated the effects of systemic B12-Ex4 and unconjugated Ex4 on food intake and body weight change, oral glucose tolerance, and nausea/malaise in male rats, and on intraperitoneal glucose tolerance in mice...
January 12, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29321828/exendin-4-protects-mice-from-d-galactose-induced-hepatic-and-pancreatic-dysfunction
#17
Akram Ahangarpour, Ali Akbar Oroojan, Mohammad Badavi
Investigations into pharmaceutical intervention of pancreatic and hepatic dysfunction associated with metabolic disturbances have received relatively little attention. The aim of this study was to investigate the protective effects of exendin-4 in mice receiving D-galactose, a reducing sugar that triggers ROS production and inflammatory mediators affecting the pancreas and liver. Exendin-4 is an United States Food and Drug Administration (FDA) approved glucagon-like peptide that increases insulin dependent glycogen synthesis and glucose uptake...
2018: Pathobiology of Aging & Age related Diseases
https://www.readbyqxmd.com/read/29317206/exendin-4-impairs-the-autophagic-flux-to-induce-apoptosis-in-pancreatic-acinar-ar42j-cells-by-down-regulating-lamp-2
#18
Zhiqiang Li, Shaihong Zhu, Lihua Huang, Mingming Shang, Can Yu, Hongwei Zhu, Duo Han, Hui Huang, Xiao Yu, Xia Li
This study aimed to explore the mechanism of impaired autophagy flux induced by exendin-4 and its role on cell apoptosis in pancreatic AR42J cells. The AR42J cells were treated with various concentration of exendin-4 for several time points to assess its cytotoxicity by MTT assay. Then the AR42J cells were treated by 10pM exendin-4 for 72 h, the cell death was analyzed by flow cytometry and caspase-3 level was examined by Western blot with or without the pretreatment of z-VAD-fmk to testify whether exendin-4 induces the cell apoptosis...
January 6, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29284659/a-targeted-rnai-screen-identifies-endocytic-trafficking-factors-that-control-glp-1-receptor-signaling-in-pancreatic-beta-cells
#19
Teresa Buenaventura, Nisha Kanda, Phoebe C Douzenis, Ben Jones, Stephen R Bloom, Pauline Chabosseau, Ivan R Corrêa, Domenico Bosco, Lorenzo Piemonti, Piero Marchetti, Paul R Johnson, Am James Shapiro, Guy A Rutter, Alejandra Tomas
The GLP-1 receptor (GLP-1R) is a key target for type 2 diabetes (T2D) treatment. Since endocytic trafficking of agonist-bound receptors is one of the most important routes for regulation of receptor signaling, a better understanding of this process may facilitate the development of new T2D therapeutic strategies. Here, we have screened 29 proteins with known functions in G protein-coupled receptor trafficking for their role in GLP-1R potentiation of insulin secretion in pancreatic beta cells. We identify five (clathrin, dynamin1, AP2, SNX27 and SNX1) that increase and four (HIP1, HIP14, GASP-1 and Nedd4) that decrease insulin secretion from murine insulinoma MIN6B1 cells in response to the GLP-1 analogue exendin-4...
December 28, 2017: Diabetes
https://www.readbyqxmd.com/read/29283509/exenatide-exhibits-anti-inflammatory-properties-and-modulates-endothelial-response-to-tumor-necrosis-factor-%C3%AE-mediated-activation
#20
Wojciech Garczorz, Enrique Gallego-Colon, Agnieszka Kosowska, Agnieszka Kłych-Ratuszny, Michał Woźniak, Wiesław Marcol, K J Niesner, Tomasz Francuz
INTRODUCTION: Cardiovascular disease is the main cause of mortality and morbidity in the industrialized world. Incretin mimetic compounds such as exenatide are currently used in the treatment of type 2 diabetes. AIMS: We investigated the effects of incretin drugs on apoptosis, adhesion molecule expression, and concentration of extracellular matrix (ECM) metalloproteinases under inflammatory conditions within the context of atherosclerotic plaque formation of both human coronary artery endothelial cells (hCAECs) and human aortic endothelial cells (hAoECs)...
December 28, 2017: Cardiovascular Therapeutics
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