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https://www.readbyqxmd.com/read/27911362/automated-acoustic-dispensing-for-the-serial-dilution-of-peptide-agonists-in-potency-determination-assays
#1
Jacqueline Naylor, Alessandra Rossi, Christopher Brankin, David C Hornigold
As with small molecule drug discovery, screening for peptide agonists requires the serial dilution of peptides to produce concentration-response curves. Screening peptides affords an additional layer of complexity as conventional tip-based sample handling methods expose peptides to a large surface area of plasticware, providing an increased opportunity for peptide loss via adsorption. Preventing excessive exposure to plasticware reduces peptide loss via adherence to plastics and thus minimizes inaccuracies in potency prediction, and we have previously described the benefits of non-contact acoustic dispensing for in vitro high-throughput screening of peptide agonists(1)...
November 10, 2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27908915/-the-hypothalamic-glucagon-like-peptide-1-glp-1-receptor-glp-1r-is-sufficient-but-not-necessary-for-the-regulation-of-energy-balance-and-glucose-homeostasis-in-mice
#2
Melissa A Burmeister, Jennifer E Ayala, Hannah Smouse, Adriana Landivar-Rocha, Jacob D Brown, Daniel J Drucker, Doris A Stoffers, Darleen A Sandoval, Randy J Seeley, Julio E Ayala
Pharmacological activation of the hypothalamic glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) promotes weight loss and improves glucose tolerance. This demonstrates that the hypothalamic GLP-1R is sufficient but does not show whether it is necessary for the effects of exogenous GLP-1R agonists (GLP-1RA) or endogenous GLP-1 on these parameters. To address this, we crossed mice harboring floxed Glp1r alleles to mice expressing Nkx2.1-Cre to knock down Glp1r expression throughout the hypothalamus (GLP-1RKD(ΔNkx2...
December 1, 2016: Diabetes
https://www.readbyqxmd.com/read/27890806/the-endocrine-disrupting-potential-of-monosodium-glutamate-msg-on-secretion-of-the-glucagon-like-peptide-1-glp-1-gut-hormone-and-glp-1-receptor-interaction
#3
Maeve Shannon, Brian Green, Gary Willars, Jodie Wilson, Natalie Matthews, Joanna Lamb, Anna Gillespie, Lisa Connolly
Monosodium glutamate (MSG) is a suspected obesogen with epidemiological evidence positively correlating consumption to increased body mass index and higher prevalence of metabolic syndrome. ELISA and high content analysis (HCA) were employed to examine the disruptive effects of MSG on the secretion of enteroendocrine hormone glucagon-like peptide-1 (GLP-1) and GLP-1 receptor (GLP-1R), respectively. Following 3h MSG exposure of the enteroendocrine pGIP/neo: STC-1 cell line model (500μg/ml) significantly increased GLP-1 secretion (1...
November 24, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/27884496/glucagon-like-peptide-1-and-its-receptor-agonists-their-roles-in-management-of-type-2-diabetes-mellitus
#4
REVIEW
Ankit Gupta, Herbert F Jelinek, Hayder Al-Aubaidy
This study summarizes major work which investigated the roles of glucagon like peptide-1 (GLP-1) and its receptor (GLP-1R); the use of GLP-1-R agonists and dipeptidyl peptidase 4 inhibitor in the management of type 2 diabetes mellitus. It focuses on the recent therapeutic development which has occurred in this field, and also discusses the potential treatments which can be discovered and implemented in the near future to design an effective therapy for type 2 diabetes mellitus.
September 15, 2016: Diabetes & Metabolic Syndrome
https://www.readbyqxmd.com/read/27880981/a-novel-glucagon-like-peptide-1-glucagon-receptor-dual-agonist-improves-steatohepatitis-and-liver-regeneration-in-mice
#5
M Pilar Valdecantos, Virginia Pardo, Laura Ruiz, Luis Castro-Sánchez, Borja Lanzón, Elisa Fernández-Millán, Carmelo García-Monzón, Ana I Arroba, Águeda González-Rodríguez, Fernando Escrivá, Álvarez Carmen, Francisco J Rupérez, Coral Barbas, Anish Konkar, Jacqui Naylor, David Hornigold, Ana Dos Santos, Maria Bednarek, Joseph Grimsby, Cristina M Rondinone, Ángela M Valverde
BACKGROUND AND AIMS: Since non-alcoholic steatohepatitis (NASH) is associated with impaired liver regeneration, we investigated the effects of G49, a dual glucagon-like peptide-1(GLP-1)/glucagon (GCG) receptor agonist, on NASH and hepatic regeneration. METHODS: C57Bl/6 mice fed chow or methionine and choline-deficient (MCD) diet for one week were divided into 4 groups: C (chow diet), MCD (MCD diet), C+G49 (chow diet plus G49) and M+G49 (MCD diet plus G49). Mice fed high fat diet (HFD) for 10 weeks were divided in groups: HFD and H+G49 (HFD plus G49)...
November 23, 2016: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/27871675/glucagon-like-peptide-1-and-the-central-peripheral-nervous-system-crosstalk-in-diabetes
#6
REVIEW
Giovanna Muscogiuri, Ralph A DeFronzo, Amalia Gastaldelli, Jens J Holst
Glucagon-like peptide-1 (GLP-1) is released in response to meals and exerts important roles in the maintenance of normal glucose homeostasis. GLP-1 is also important in the regulation of neurologic and cognitive functions. These actions are mediated via neurons in the nucleus of the solitary tract that project to multiple regions expressing GLP-1 receptors (GLP-1Rs). Treatment with GLP-1R agonists (GLP-1-RAs) reduces ischemia-induced hyperactivity, oxidative stress, neuronal damage and apoptosis, cerebral infarct volume, and neurologic damage, after cerebral ischemia, in experimental models...
October 27, 2016: Trends in Endocrinology and Metabolism: TEM
https://www.readbyqxmd.com/read/27856285/neurotrophic-and-neuroprotective-effects-of-oxyntomodulin-in-neuronal-cells-and-a-rat-model-of-stroke
#7
Yazhou Li, Kou-Jen Wu, Seong-Jin Yu, Ian A Tamargo, Yun Wang, Nigel H Greig
Proglucagon-derived peptides, especially glucagon-like peptide-1 (GLP-1) and its long-acting mimetics, have exhibited neuroprotective effects in animal models of stroke. Several of these peptides are in clinical trials for stroke. Oxyntomodulin (OXM) is a proglucagon-derived peptide that co-activates the GLP-1 receptor (GLP-1R) and the glucagon receptor (GCGR). The neuroprotective action of OXM, however, has not been thoroughly investigated. In this study, the neuroprotective effect of OXM was first examined in human neuroblastoma (SH-SY5Y) cells and rat primary cortical neurons...
November 14, 2016: Experimental Neurology
https://www.readbyqxmd.com/read/27845037/novel-glp-1r-gipr-co-agonist-twincretin-is-neuroprotective-in-cell-and-rodent-models-of-mild-traumatic-brain-injury
#8
Ian A Tamargo, Miaad Bader, Yazhou Li, Seong-Jin Yu, Yun Wang, Konrad Talbot, Richard D DiMarchi, Chaim G Pick, Nigel H Greig
Several single incretin receptor agonists that are approved for the treatment of type 2 diabetes mellitus (T2DM) have been shown to be neuroprotective in cell and animal models of neurodegeneration. Recently, a synthetic dual incretin receptor agonist, nicknamed "twincretin," was shown to improve upon the metabolic benefits of single receptor agonists in mouse and monkey models of T2DM. In the current study, the neuroprotective effects of twincretin are probed in cell and mouse models of mild traumatic brain injury (mTBI), a prevalent cause of neurodegeneration in toddlers, teenagers and the elderly...
November 11, 2016: Experimental Neurology
https://www.readbyqxmd.com/read/27832483/7tm-domain-structure-of-adhesion-gpcrs
#9
Chris de Graaf, Saskia Nijmeijer, Steffen Wolf, Oliver P Ernst
Schematic presentation of the overall adhesion G Protein-Coupled Receptor (aGPCR) structure and functional domains, covering an extracellular N-terminal fragment (NTF), a membrane-spanning C-terminal fragment (CTF) and a GPCR proteolysis site (GPS). (Left side) aGPCR model constructed based on the seven-transmembrane (7TM) structure (blue) of secretin family glucagon receptor (GCGR) (PDB, 4L6R) [11] and the GPCR autoproteolysis inducing (GAIN) domain (magenta) structure of latrophilin 1 (PDB, 4DLQ) [9]...
2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27823886/helixconstraints-and-amino-acid-substitution-in-glp-1-increase-camp-and-insulin-secretion-but-not-beta-arrestin-2-signaling
#10
Fabien Plisson, Timothy A Hill, Justin M Mitchell, Huy N Hoang, Aline D de Araujo, Weijun Xu, Adam Cotterell, David J Edmonds, Robert V Stanton, David R Derksen, Paula M Loria, David A Griffith, David A Price, Spiros Liras, David P Fairlie
Glucagon-like peptide (GLP-1) is an endogenous hormone that induces insulin secretion from pancreatic islets and modified forms are used to treat diabetes mellitus type 2. Understanding how GLP-1 interacts with its receptor (GLP-1R) can potentially lead to more effective drugs. Modeling and NMR studies of the N-terminus of GLP-1 suggest a β-turn between residues Glu9-Phe12 and a kinked alpha helix between Val16-Gly37. N-terminal turn constraints attenuated binding affinity and activity (compounds 1-8). Lys-Asp (i, i+4) crosslinks in the middle and at the C-terminus increased alpha helicity and cAMP stimulation without much effect on binding affinity or beta-arrestin 2 recruitment (compounds 9-18)...
October 21, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27813409/%C3%AE-arrestin-biased-agonists-of-the-glp-1-receptor-from-%C3%AE-amino-acid-residue-incorporation-into-glp-1-analogues
#11
Marlies V Hager, Lisa M Johnson, Denise Wootten, Patrick M Sexton, Samuel H Gellman
Activation of a G protein-coupled receptor (GPCR) causes recruitment of multiple intracellular proteins, each of which can activate distinct signaling pathways. This complexity has engendered interest in agonists that preferentially stimulate subsets among the natural signaling pathways ("biased agonists"). We have examined analogues of glucagon-like peptide-1 (GLP-1) containing β-amino acid residues in place of native α residues at selected sites and found that some analogues differ from GLP-1 in terms of their relative abilities to promote G protein activation (as monitored via cAMP production) versus β-arrestin recruitment (as monitored via BRET assays)...
November 4, 2016: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/27802600/comparison-of-regulation-mechanisms-of-five-mulberry-ingredients-on-insulin-secretion-under-oxidative-stress
#12
Yun-Chong Zheng, Hao He, Xing Wei, Sheng Ge, Yan-Hua Lu
The effects of mulberry ingredients including 1-deoxynojrimycin (DNJ), resveratrol (RES), oxyresveratrol (OXY), cyanidin-3-glucoside (C3G), and cyanidin-3-rutinoside (C3R) on insulin secretion under oxidative stress were investigated. The results revealed that they had distinct effects on insulin secretion in H2O2-induced MIN 6 cells, especially DNJ, C3G and C3R, While RES and OXY showed modest effects in low dose (12.5μM). The mechanisms were demonstrated in signal pathway that after treatment with DNJ, C3G and C3R, the expressions of glucokinase (GK) were up-regulated, leading to intracellular ATP accumulation and insulin secretion...
November 1, 2016: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/27784780/exendin-4-ameliorates-lipotoxicity-induced-glomerular-endothelial-cell-injury-by-improving-abc-transporter-a1-mediated-cholesterol-efflux-in-diabetic-apoe-knockout-mice
#13
Qing-Hua Yin, Rui Zhang, Li Li, Yi-Ting Wang, Jing-Ping Liu, Jie Zhang, Lin Bai, Jing-Qiu Cheng, Ping Fu, Fang Liu
The ATP-binding cassette transporter A1 (ABCA1), which promotes cholesterol efflux from cells and inhibits inflammatory responses, is highly expressed in the kidney. Research has shown that exendin-4, a glucagon-like peptide-1 receptor (GLP-1R) agonist, promotes ABCA1 expression in multiple tissues and organs; however, the mechanisms underlying exendin-4 induction of ABCA1 expression in glomerular endothelial cells are not fully understood. In this study we investigated the effect of exendin-4 on ABCA1 in glomerular endothelial cells of diabetic kidney disease (DKD) and the possible mechanism...
October 26, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27782127/endogenous-glucagon-like-peptide-1-receptor-signaling-in-the-nucleus-tractus-solitarius-is-required-for-food-intake-control
#14
Amber L Alhadeff, Blake D Mergler, Derek J Zimmer, Christopher A Turner, David J Reiner, Heath D Schmidt, Harvey J Grill, Matthew R Hayes
Though the glucagon-like peptide-1 (GLP-1) system is critical to energy balance control and is a target for obesity pharmacotherapies, the receptor populations mediating effects of endogenous GLP-1 signaling are not fully understood. To address this, we developed a novel adeno-associated virus (AAV-GLP-1R) that utilizes short hairpin RNA to chronically knock down GLP-1 receptors (GLP-1R) in rats. Since pharmacological studies highlight the hindbrain nucleus tractus solitarius (NTS) as a brain region important for GLP-1R-mediated effects on energy balance, AAV-GLP-1R was injected into the NTS to examine the role of endogenous NTS GLP-1R signaling in energy balance control...
October 26, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27780892/diabetes-negatively-affects-cortical-and-striatal-gabaergic-neurons-an-effect-that-is-partially-counteracted-by-exendin-4
#15
Martin Larsson, Grazyna Lietzau, David Nathanson, Claes-Göran Östenson, Carina Mallard, Maria E Johansson, Thomas Nyström, Cesare Patrone, Vladimer Darsalia
Type 2 diabetic (T2D) patients often develop early cognitive and sensorimotor impairments. The pathophysiological mechanisms behind these problems are largely unknown. Recent studies demonstrate that dysfunctional γ-Aminobutyric acid (GABAergic) neurons are involved in age-related cognitive decline. We hypothesized that similar, but earlier dysfunction is taking place under T2D in the neocortex and striatum (two brain areas important for cognition and sensorimotor functions). We also hypothesized that the T2D-induced effects are pharmacologically reversible by anti-diabetic drugs targeting the glucagon-like peptide-1 receptor (GLP-1R)...
October 25, 2016: Bioscience Reports
https://www.readbyqxmd.com/read/27746194/is-cleaved-glucagon-like-peptide-1-really-inactive-effects-of-glp-1-9-36-on-human-adipose-stem-cells
#16
Giulia Cantini, Alessandra Di Franco, Edoardo Mannucci, Michaela Luconi
Glucagon-like peptide 1(9-36) [GLP-1(9-36)] is generated by dipeptidyl peptidase-4 (DPP4) cleavage of the gut incretin hormone, GLP-1(7-36). Since GLP-1(9-36) has a very low affinity for the GLP-1 receptor (GLP-1R), it has so far been considered an inactive form of GLP-1. Here we show GLP-1(9-36) activity in human adipose stem cells (ASC) in vitro. GLP-1(9-36) inhibits human ASC proliferation, glucose uptake and adipogenesis, as well as induces cell apoptosis, to a similar extent as GLP-1(7-36) and liraglutide...
October 13, 2016: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/27732058/vascular-biology-of-glucagon-receptor-superfamily-peptides-complexity-controversy-and-clinical-relevance
#17
Gemma Pujadas, Daniel J Drucker
Regulatory peptides produced in islet and gut endocrine cells, including glucagon, GLP-1, GLP-2, and GIP exert actions with considerable metabolic importance and translational relevance. Although the clinical development of GLP-1 receptor (GLP-1R) agonists and dipeptidyl peptidase-4(DPP4) inhibitors has fostered research into how these hormones act on the normal and diseased heart, less is known about the actions of these peptides on blood vessels. Here we review the effects of these peptide hormones on normal blood vessels, and highlight their vascular actions in the setting of experimental and clinical vascular injury...
October 12, 2016: Endocrine Reviews
https://www.readbyqxmd.com/read/27721184/liraglutide-promotes-improvements-in-objective-measures-of-cognitive-dysfunction-in-individuals-with-mood-disorders-a-pilot-open-label-study
#18
Rodrigo B Mansur, Juhie Ahmed, Danielle S Cha, Hanna O Woldeyohannes, Mehala Subramaniapillai, Julie Lovshin, Jung G Lee, Jae-Hon Lee, Elisa Brietzke, Eva Z Reininghaus, Kang Sim, Maj Vinberg, Natalie Rasgon, Tomas Hajek, Roger S McIntyre
BACKGROUND: There is a paucity of treatments that are capable of reliably and robustly improving cognitive function in adults with mood disorders. Glucagon-like peptide-1 is synthesized centrally and its receptors are abundantly expressed in neural circuits subserving cognitive function. We aimed to determine the effects of liraglutide, a GLP-1 receptor (GLP-1R) agonist, on objective measures of cognition in adults with a depressive or bipolar disorder. METHODS: In this 4-week, pilot, open-label, domain-based study (e...
January 1, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/27702763/glucagon-like-peptide-1-glp-1-mediates-cardioprotection-by-remote-ischaemic-conditioning
#19
Marina V Basalay, Svetlana Mastitskaya, Aleksander Mrochek, Gareth L Ackland, Ana Gutierrez Del Arroyo, Jenifer Sanchez, Per-Ove Sjoquist, John Pernow, Alexander V Gourine, Andrey Gourine
AIMS: Although the nature of the humoral factor which mediates cardioprotection established by remote ischaemic conditioning (RIc) remains unknown, parasympathetic (vagal) mechanisms appear to play a critical role. As the production and release of many gut hormones is modulated by the vagus nerve, here we tested the hypothesis that RIc cardioprotection is mediated by the actions of glucagon-like peptide-1 (GLP-1). METHODS AND RESULTS: A rat model of myocardial infarction (coronary artery occlusion followed by reperfusion) was used...
October 4, 2016: Cardiovascular Research
https://www.readbyqxmd.com/read/27698937/activation-of-glp-1-receptor-enhances-neuronal-base-excision-repair-via-pi3k-akt-induced-expression-of-apurinic-apyrimidinic-endonuclease-1
#20
Jenq-Lin Yang, Wei-Yu Chen, Yin-Ping Chen, Chao-Ying Kuo, Shang-Der Chen
Glucagon-like peptide-1 (GLP-1) is an intestinal-secreted incretin that increases cellular glucose up-take to decrease blood sugar. Recent studies, however, suggest that the function of GLP-1 is not only to decrease blood sugar, but also acts as a neurotrophic factor that plays a role in neuronal survival, neurite outgrowth, and protects synaptic plasticity and memory formation from effects of β-amyloid. Oxidative DNA damage occurs during normal neuron-activity and in many neurological diseases. Our study describes how GLP-1 affected the ability of neurons to ameliorate oxidative DNA damage...
2016: Theranostics
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