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https://www.readbyqxmd.com/read/29226686/enhanced-specific-activity-by-multi-chelation-of-exendin-3-leads-to-improved-image-quality-and-in-vivo-beta-cell-imaging
#1
Lieke Joosten, Maarten Brom, Hanneke Peeters, Sandra Heskamp, Martin Behe, Otto C Boerman, Martin Gotthardt
OBJECTIVE: Glucagon like peptide-1 receptor (GLP-1R) targeting using radiolabeled exendin is a promising approach to non-invasively visualize and determine beta cell mass (BCM), which could help to unravel the pathophysiology of diabetes. However, saturation of the GLP-1R on beta cells occurs at low peptide doses, since the number of receptors expressed under physiological conditions is low. Therefore, tracers with high specific activities are required to sensitively image small variations in BCM...
December 11, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29221794/glp-1-action-in-the-mouse-bed-nucleus-of-the-stria-terminalis
#2
Diana L Williams, Nicole A Lilly, Ian J Edwards, Pallas Yao, James E Richards, Stefan Trapp
Glucagon-like peptide-1 (GLP-1) injected into the brain reduces food intake. Similarly, activation of preproglucagon (PPG) cells in the hindbrain which synthesize GLP-1, reduces food intake. However, it is far from clear whether this happens because of satiety, nausea, reduced reward, or even stress. Here we explore the role of the bed nucleus of the stria terminalis (BNST), an area involved in feeding control as well as stress responses, in GLP-1 responses. Using cre-expressing mice we visualized projections of NTS PPG neurons and GLP-1R-expressing BNST cells with AAV-driven Channelrhodopsin-YFP expression...
December 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29200876/effects-of-insulin-analogs-and-glucagon-like-peptide-1-receptor-agonists-on-proliferation-and-cellular-energy-metabolism-in-papillary-thyroid-cancer
#3
Liang He, Siliang Zhang, Xiaowen Zhang, Rui Liu, Haixia Guan, Hao Zhang
Purpose: This study was aimed to investigate the expressions of the insulin receptor (IR), insulin-like growth factor receptor (IGF-1R), and glucagon-like peptide-1 receptor (GLP-1R) in normal thyroid tissue, papillary thyroid cancer (PTC) tissues, and PTC cells, and to examine the possible role of insulin analogs and GLP-1R agonists in cell proliferation and energy metabolism in PTC cells. Methods: The expressions of IR, IGF-1R, and GLP-1R in PTC tissues and PTC cell lines were detected by immunohistochemistry and western blotting, respectively...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29200726/influence-of-flavonoids-on-mechanism-of-modulation-of-insulin-secretion
#4
Juliana Mikaelly Dias Soares, Ana Ediléia Barbosa Pereira Leal, Juliane Cabral Silva, Jackson R G S Almeida, Helinando Pequeno de Oliveira
Background: The development of alternatives for insulin secretion control in vivo or in vitro represents an important aspect to be investigated. In this direction, natural products have been progressively explored with this aim. In particular, flavonoids are potential candidates to act as insulin secretagogue. Objective: To study the influence of flavonoid on overall modulation mechanisms of insulin secretion. Methods: The research was conducted in the following databases and platforms: PubMed, Scopus, ISI Web of Knowledge, SciELO, LILACS, and ScienceDirect, and the MeSH terms used for the search were flavonoids, flavones, islets of Langerhans, and insulin-secreting cells...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29193738/cooperative-role-of-the-glp-1-receptor-and-%C3%AE-3-adrenergic-mediated-signaling-on-fat-mass-reduction-through-the-down-regulation-of-pka-akt-ampk-signaling-in-the-adipose-tissue-and-muscle-of-rats
#5
Juan Decara, Patricia Rivera, Sergio Arrabal, Antonio Vargas, Antonia Serrano, Francisco Javier Pavón, Carlos Dieguez, Rubén Nogueiras, Fernando Rodríguez de Fonseca, Juan Suárez
AIM: To explore the cooperation of GLP-1 receptor and β3-adrenergic receptor-mediated signaling in the control of fat mass/feeding behavior by studying the effects of a combined therapy composed of the GLP-1R agonist liraglutide and the β3-AR agonist CL316243. METHODS: The study included the analysis of key mechanisms regulating lipid/cholesterol metabolism, and thermogenesis in brown (BAT) and epididymal white (eWAT) adipose tissues, abdominal muscle and liver of male rats...
November 28, 2017: Acta Physiologica
https://www.readbyqxmd.com/read/29193450/clostridium-butyricum-exerts-a-neuroprotective-effect-in-a-mouse-model-of-traumatic-brain-injury-via-the-gut-brain-axis
#6
H Li, J Sun, J Du, F Wang, R Fang, C Yu, J Xiong, W Chen, Z Lu, J Liu
BACKGROUND: Traumatic brain injury (TBI) is a common occurrence following gastrointestinal dysfunction. Recently, more and more attentions are being focused on gut microbiota in brain and behavior. Glucagon-like peptide-1 (GLP-1) is considered as a mediator that links the gut-brain axis. The aim of this study was to explore the neuroprotective effects of Clostridium butyricum (Cb) on brain damage in a mouse model of TBI. METHODS: Male C57BL/6 mice were subjected to a model of TBI-induced by weight-drop impact head injury and were treated intragastrically with Cb...
November 27, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/29177486/glucagon-like-peptide-1-inhibits-prandial-gastrointestinal-motility-through-myenteric-neuronal-mechanisms-in-humans
#7
Md Abdul Halim, Marie Degerblad, Magnus Sundbom, Urban Karlbom, Jens Juul Holst, Dominic-Luc Webb, Per M Hellström
Context: Glucagon-like peptide-1 (GLP-1) secretion from L-cells and postprandial inhibition of gastrointestinal motility. Objective: Investigate whether physiological plasma concentrations of GLP-1 can inhibit human postprandial gastrointestinal motility; determine target mechanism of GLP-1 and analogue ROSE-010 action. Design: Single-blind parallel study. Setting: University research laboratory. Participants: Healthy volunteers investigated with antroduodenojejunal manometry...
November 21, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29175324/lixisenatide-reduces-amyloid-plaques-neurofibrillary-tangles-and-neuroinflammation-in-an-app-ps1-tau-mouse-model-of-alzheimer-s-disease
#8
Hong-Yan Cai, Jun-Ting Yang, Zhao-Jun Wang, Jun Zhang, Wei Yang, Mei-Na Wu, Jin-Shun Qi
Type 2 diabetes mellitus (T2DM) has been identified as a high risk factor for Alzheimer's disease (AD). The impairment of insulin signaling has been found in AD brain. Glucagon-like peptide-1 (GLP-1) is an incretin hormone, normalises insulin signaling and acts as a neuroprotective growth factor. We have previously shown that the long-lasting GLP-1 receptor (GLP-1R) agonist lixisenatide plays an important role in memory formation, synaptic plasticity and cell proliferation of rats. In the follow-up study, we analysed the neuroprotective effect and mechanism of lixisenatide, injected for 60 days at 10 nmol/kg i...
November 21, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29156769/liraglutide-activates-autophagy-via-glp-1r-to-improve-functional-recovery-after-spinal-cord-injury
#9
Jian Chen, Zhouguang Wang, Yuqin Mao, Zengming Zheng, Yu Chen, Sinan Khor, Kesi Shi, Zili He, Jiawei Li, Fanghua Gong, Yanlong Liu, Aiping Hu, Jian Xiao, Xiangyang Wang
Therapeutics used to treat central nervous system (CNS) injury are designed to promote axonal regeneration and inhibit cell death. Previous studies have shown that liraglutide exerts potent neuroprotective effects after brain injury. However, little is known if liraglutide treatment has neuroprotective effects after spinal cord injury (SCI). This study explores the neuroprotective effects of liraglutide and associated underlying mechanisms. Our results showed that liraglutide could improve recovery after injury by decreasing apoptosis as well as increasing microtubulin acetylation, and autophagy...
October 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29136785/obestatin-prevents-h2o2-induced-damage-through-activation-of-trkb-in-rgc-5-cells
#10
Yang Liu, Yue-Xian Xing, Xin-Yuan Gao, Hong-Yu Kuang, Jing Zhang, Rong Liu
BACKGROUD: In the early stage of diabetic retinopathy, the damage of retinal ganglion cells already exists, promoting the development of the disease. The aim of this study was to investigate the protective role and the mechanisms of obestatin against H2O2-induced damage in RGC-5 cells. METHODS: RGC-5 cells were incubated with various concentrations of obestatin for 24h before H2O2 added. The survival rates of RGC-5 were measured by MTT assay. The expression of apoptosis-related proteins and TrkB pathway-related proteins were detected by Western blot analysis...
November 8, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29113464/a-new-treatment-strategy-for-parkinson-s-disease-through-the-gut-brain-axis-the-glucagon-like-peptide-1-receptor-pathway
#11
Dong Seok Kim, Ho-Il Choi, Yun Wang, Yu Luo, Barry J Hoffer, Nigel H Greig
Molecular communications in the gut-brain axis, between the central nervous system and the gastrointestinal tract, are critical for maintaining healthy brain function, particularly in aging. Epidemiological analyses indicate type 2 diabetes mellitus (T2DM) is a risk factor for neurodegenerative disorders including Alzheimer's disease (AD) and Parkinson's diseases (PD) for which aging shows a major correlative association. Common pathophysiological features exist between T2DM, AD, and PD, including oxidative stress, inflammation, insulin resistance, abnormal protein processing, and cognitive decline, and suggest that effective drugs for T2DM that positively impact the gut-brain axis could provide an effective treatment option for neurodegenerative diseases...
September 2017: Cell Transplantation
https://www.readbyqxmd.com/read/29110715/liraglutide-dictates-macrophage-phenotype-in-apolipoprotein-e-null-mice-during-early-atherosclerosis
#12
Robyn Bruen, Sean Curley, Sarina Kajani, Daniel Crean, Marcella E O'Reilly, Margaret B Lucitt, Catherine G Godson, Fiona C McGillicuddy, Orina Belton
BACKGROUND: Macrophages play a pivotal role in atherosclerotic plaque development. Recent evidence has suggested the glucagon-like peptide-1 receptor (GLP-1R) agonist, liraglutide, can attenuate pro-inflammatory responses in macrophages. We hypothesized that liraglutide could limit atherosclerosis progression in vivo via modulation of the inflammatory response. METHODS: Human THP-1 macrophages and bone marrow-derived macrophages, from both wild-type C57BL/6 (WT) and apolipoprotein E null mice (ApoE(-/-)) were used to investigate the effect of liraglutide on the inflammatory response in vitro...
November 6, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/29107284/superior-reductions-in-hepatic-steatosis-and-fibrosis-with-co-administration-of-a-glucagon-like-peptide-1-receptor-agonist-and-obeticholic-acid-in-mice
#13
Hani Jouihan, Sarah Will, Silvia Guionaud, Michelle L Boland, Stephanie Oldham, Peter Ravn, Anthony Celeste, James L Trevaskis
OBJECTIVE: Nonalcoholic steatohepatitis (NASH) is an unmet need associated with metabolic syndrome. There are no approved therapies for NASH; however, glucagon-like peptide-1 receptor (GLP-1R) and farnesoid-X receptor (FXR) agonists are promising drug targets. We investigated the therapeutic effects of co-administration of a GLP-1R agonist, IP118, with FXR agonist obeticholic acid (OCA) in mice. METHODS: OCA and IP118 alone and in combination were sub-chronically administered to Lep(ob)/Lep(ob) mice with diet-induced NASH or diet-induced obese (DIO) mice...
November 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/29107282/the-autonomic-nervous-system-and-cardiac-glp-1-receptors-control-heart-rate-in-mice
#14
Laurie L Baggio, John R Ussher, Brent A McLean, Xiemin Cao, M Golam Kabir, Erin E Mulvihill, Alexandra S Mighiu, Hangjun Zhang, Andreas Ludwig, Randy J Seeley, Scott P Heximer, Daniel J Drucker
OBJECTIVES: Glucagon-like peptide-1 (GLP-1) is secreted from enteroendocrine cells and exerts a broad number of metabolic actions through activation of a single GLP-1 receptor (GLP-1R). The cardiovascular actions of GLP-1 have garnered increasing attention as GLP-1R agonists are used to treat human subjects with diabetes and obesity that may be at increased risk for development of heart disease. Here we studied mechanisms linking GLP-1R activation to control of heart rate (HR) in mice...
November 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/29104476/glp-1-treatment-improves-diabetic-retinopathy-by-alleviating-autophagy-through-glp-1r-erk1-2-hdac6-signaling-pathway
#15
Xiangsheng Cai, Jingjing Li, Mingzhu Wang, Miaoqin She, Yongming Tang, Jinlong Li, Hongwei Li, Hongxiang Hui
Objective: Apoptosis and autophagy of retinal cells, which may be induced by oxidative stress, are tightly associated with the pathogenesis of diabetic retinopathy (DR). The autophagy induced by oxidative stress is considered as excessively stimulated autophagy, which accelerates the progression of DR. This study aims to investigate the protective effect of GLP-1 treatment on alleviating apoptosis and autophagy of retinal cells in type 2 diabetic rats and reveals its possible mechanism. Methods: Type 2 diabetic rats were induced by fed with high sugar, high fat diet and followed with streptozotocin injection...
2017: International Journal of Medical Sciences
https://www.readbyqxmd.com/read/29095968/characterization-of-the-glucagon-like-peptide-1-receptor-in-male-mouse-brain-using-a-novel-antibody-and-in-situ-hybridization
#16
Casper Bo Jensen, Charles Pyke, Morten Grønbech Rasch, Anders Bjorholm Dahl, Lotte Bjerre Knudsen, Anna Secher
Glucagon-like peptide-1 (GLP-1) is a physiological regulator of appetite and long-acting GLP-1 receptor agonists (GLP-1RA) lower food intake and bodyweight in both human and animal studies. The effects are mediated through brain GLP-1Rs, and several brain nuclei expressing the GLP-1R may be involved. To date, mapping the complete location of GLP-1R protein in the brain has been challenged by lack of good antibodies and the discrepancy between mRNA and protein especially relevant in neuronal axonal processes...
October 30, 2017: Endocrinology
https://www.readbyqxmd.com/read/29091882/incretin-hormones-receptor-signaling-plays-the-key-role-in-antidiabetic-potential-of-pty-2-against-stz-induced-pancreatitis
#17
Shivani Srivastava, Priya Shree, Harsh Pandey, Yamini Bhusan Tripathi
AIMS: Incretin therapy is one of the most potential approaches in the treatment of diabetes. In contrast to markedly available drugs, the herbal incretin modulators have lesser side effects with low economic cost. The main aim of this work was to analyze the potential of previously reported DPPIV inhibitor, aqueous extract of Pueraria tuberosa tubers (PTY-2) as incretin hormones receptor agonist against streptozotocin (STZ)-induced diabetes. METHODS: Chronic diabetes was induced with STZ (65mg/kg bw) in rats for 60days and grouped into diabetic control and PTY-2...
October 26, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29089613/glp-1-and-igf-i-levels-are-elevated-in-late-infancy-in-low-birthweight-infants-independently-of-glp-1-receptor-polymorphisms-and-neonatal-nutrition
#18
M Díaz, C García-Beltran, A López-Bermejo, F de Zegher, L Ibáñez
Low birth weight followed by rapid postnatal weight gain is associated with increased risks for obesity and diabetes in adulthood. Modulation of glucagon-like-peptide 1 (GLP-1) secretion by (epi)genetic mechanisms or nutrition may influence in part this risk. Formula fed infants born small-for-gestational-age (SGA) have higher circulating GLP-1 at age 4 months than breastfed SGA or appropriate-for-gestational-age (AGA) infants. Here, we assessed GLP-1 concentrations in healthy AGA (n=149) and SGA (n=107) subjects at age 12 months, and their association with endocrine-metabolic and body composition parameters and GLP-1 receptor (GLP-1R) rs6923761 and rs3765467 polymorphisms...
November 1, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/29074015/les-%C3%A2-nouvelles-%C3%A2-classes-d-antidiab%C3%A3-tiques-consid%C3%A3-rations-ophtalmologiques-relatives-aux-agonistes-du-glp-1r-aux-inhibiteurs-de-la-dpp-4-et-aux-inhibiteurs-du-sglt2
#19
EDITORIAL
Kylen D McReelis, Julie A Lovshin
No abstract text is available yet for this article.
November 2017: Canadian Journal of Ophthalmology. Journal Canadien D'ophtalmologie
https://www.readbyqxmd.com/read/29074013/newer-classes-of-antidiabetes-drugs-ophthalmological-considerations-for-glp-1r-agonists-dpp-4-inhibitors-and-sglt-2-inhibitors
#20
EDITORIAL
Kylen D McReelis, Julie A Lovshin
No abstract text is available yet for this article.
November 2017: Canadian Journal of Ophthalmology. Journal Canadien D'ophtalmologie
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