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Glp 1 agonist

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https://www.readbyqxmd.com/read/27917122/glucagon-like-peptide-1-analog-liraglutide-delays-onset-of-experimental-autoimmune-encephalitis-in-lewis-rats
#1
Brian DellaValle, Gitte S Brix, Birgitte Brock, Michael Gejl, Anne M Landau, Arne Møller, Jørgen Rungby, Agnete Larsen
Introduction: Recent findings indicate that metabolic disturbances are involved in multiple sclerosis (MS) pathology and influence the susceptibility to treatment, directing attention toward anti-diabetic drugs such as metformin and pioglitazone. Liraglutide, a drug of the glucagon-like peptide-1 (GLP-1) family, is also anti-diabetic and weight-reducing and is, moreover, directly neuroprotective and anti-inflammatory in a broad spectrum of experimental models of brain disease. In this study we investigate the potential for this FDA-approved drug, liraglutide, as a treatment for MS by utilizing the experimental model, experimental autoimmune encephalitis (EAE)...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27913575/lowest-glucose-variability-and-hypoglycemia-are-observed-with-the-combination-of-a-glp-1-receptor-agonist-and-basal-insulin-variation-study
#2
Harpreet S Bajaj, Karri Venn, Chenglin Ye, Avril Patrick, Shivani Kalra, Hasnain Khandwala, Nadeem Aslam, David Twum-Barima, Ronnie Aronson
OBJECTIVE: There is a dearth of published literature comparing glucose variability (GV) between different insulin regimens in type 2 diabetes. This cohort study compares GV using continuous glucose monitoring (CGM) in patients with well-controlled type 2 diabetes using four common insulin regimens: basal insulin + oral drugs (BO), basal insulin + glucagon-like peptide 1 receptor agonist (GLP-1 RA) (BGLP), premixed insulin (PM), and basal-bolus insulin (BB). RESEARCH DESIGN AND METHODS: Consecutive patients from three endocrinology clinics who met study criteria-type 2 diabetes, age 18 to 80 years, BMI ≤ 45 kg/m(2), stable insulin regimen for a minimum of 6 months, and stable A1C value ≤7...
December 2, 2016: Diabetes Care
https://www.readbyqxmd.com/read/27911362/automated-acoustic-dispensing-for-the-serial-dilution-of-peptide-agonists-in-potency-determination-assays
#3
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
#4
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/27908836/gq-and-gs-signaling-acting-in-synergy-to-control-glp-1-secretion
#5
Maria Hauge, Jeppe Pio Ekberg, Maja Storm Engelstoft, Pascal Timshel, Andreas N Madsen, Thue W Schwartz
GPR40 is generally known to signal through Gq. However, in transfected cells, certain synthetic agonists can make the receptor signal also through Gs and cAMP (Hauge et al., 2015). Here we find that, in colonic crypt cultures, the GLP-1 secretion induced by such Gq + Gs GPR40 agonists is indeed inhibited by blockers of both Gq and Gs and is eliminated by combining these. This in contrast to Gq-only GPR40 agonists which only are affected by the Gq inhibitor. Importantly, Gq-only GPR40 agonists in combination with low doses of selective synthetic agonists for Gs coupled receptors, e...
November 28, 2016: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/27889301/glycemic-control-and-weight-outcomes-for-exenatide-once-weekly-versus-liraglutide-in-patients-with-type-2-diabetes-a-1-year-retrospective-cohort-analysis
#6
Carrie McAdam-Marx, Hiep Nguyen, Marisa B Schauerhamer, Mukul Singhal, Sudhir Unni, Xiangyang Ye, David Cobden
PURPOSE: Data comparing real-world effectiveness of the glucagon-like peptide-1 receptor agonists (GLP-1RAs) exenatide once weekly (QW) and liraglutide in the treatment of type 2 diabetes (T2D) are limited. Furthermore, there is limited information on exenatide QW or liraglutide response by glycemic control and insulin use status. This study identifies 1-year glycosylated hemoglobin (HbA1c) and weight outcomes with exenatide QW and liraglutide in the real-world setting overall and in insulin-naive patients with uncontrolled T2D...
November 23, 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/27884660/exenatide-improves-diastolic-function-and-attenuates-arterial-stiffness-but-does-not-alter-exercise-capacity-in-individuals-with-type-2-diabetes
#7
Rebecca L Scalzo, Kerrie L Moreau, Cemal Ozemek, Leah Herlache, Shawna McMillin, Sarah Gilligan, Amy G Huebschmann, Tim A Bauer, Jennifer Dorosz, Jane E B Reusch, Judith G Regensteiner
BACKGROUND: Exercise is recommended as a cornerstone of treatment for type 2 diabetes mellitus (T2DM), however, it is often poorly adopted by patients. Even in the absence of apparent cardiovascular disease, persons with T2DM have an impaired ability to carry out maximal and submaximal exercise and these impairments are correlated with cardiac and endothelial dysfunction. Glucagon-like pepetide-1 (GLP-1) augments endothelial and cardiac function in T2DM. We hypothesized that administration of a GLP-1 agonist (exenatide) would improve exercise capacity in T2DM...
October 7, 2016: Journal of Diabetes and its Complications
https://www.readbyqxmd.com/read/27884496/glucagon-like-peptide-1-and-its-receptor-agonists-their-roles-in-management-of-type-2-diabetes-mellitus
#8
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
#9
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/27879196/treatment-persistence-in-the-use-of-basal-insulins-in-poland-and-germany%C3%A2
#10
Wolfgang Rathmann, Marcin Czech, Edward Franek, Karel Kostev
AIMS: To compare short-term basal insulin therapy persistence and its predictors in Poland and Germany. METHODS: Persistence was defined as proportions of patients remaining on the initial basal insulin (analogs: Poland: n = 6,889, Germany: n = 454,067; neutral protamine Hagedorn (NPH) insulins: Poland: n = 50,761, Germany: n = 226,064) over 2 years based on nationwide prescription databases (LRx; IMS Health) in Poland and Germany from 2013 to 2015. Persistence was evaluated by Kaplan-Meier curves (log-rank tests)...
November 23, 2016: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27878229/glucagon-like-peptide-1-improves-insulin-resistance-in-vitro-through-anti-inflammation-of-macrophages
#11
C Guo, T Huang, A Chen, X Chen, L Wang, F Shen, X Gu
Glucagon-like peptide 1 (GLP-1), a kind of gut hormone, is used in the treatment of type 2 diabetes (T2D). Emerging evidence indicates that GLP-1 has anti-inflammatory activity. Chronic inflammation in the adipose tissue of obese individuals is a cause of insulin resistance and T2D. We hypothesized that GLP-1 analogue therapy in patients with T2D could suppress the inflammatory response of macrophages, and therefore inhibit insulin resistance. Our results showed that GLP-1 agonist (exendin-4) not only attenuated macrophage infiltration, but also inhibited the macrophage secretion of inflammatory cytokines including TNF-β, IL-6, and IL-1β...
November 21, 2016: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/27875915/efficacy-and-safety-of-insulin-glp-1-receptor-agonists-combination-in-type-2-diabetes-mellitus-a-systematic-review
#12
D Cimmaruta, M I Maiorino, C Scavone, L Sportiello, F Rossi, D Giugliano, K Esposito, A Capuano
Attaining optimal glycemic targets in patients with type 2 diabetes is often hard and compromised by the shortcomings of the several treatments. Areas covered: When glycemic levels are not adequately controlled, an association of GLP-1 receptor agonists and insulin therapy can be adopted. In order to assess the benefit/risk profile of this combination therapy, a literature search of randomized clinical trials was performed.Eighteen trials matched the inclusion criteria. In 10 studies, GLP-1 receptor agonists were added on to an existing regimen, whereas insulin added to an existing GLP-1 receptor agonists regimen occurred in 2 studies...
December 2016: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/27871675/glucagon-like-peptide-1-and-the-central-peripheral-nervous-system-crosstalk-in-diabetes
#13
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/27868372/liraglutide-as-adjunct-to-insulin-treatment-in-type-1-diabetes-does-not-interfere-with-glycaemic-recovery-or-gastric-emptying-rate-during-hypoglycaemia-a-randomised-placebo-controlled-double-blind-parallel-group-study
#14
Christian Seerup Frandsen, Thomas Fremming Dejgaard, Henrik Ullits Andersen, Jens Juul Holst, Bolette Hartmann, Birger Thorsteinsson, Sten Madsbad
AIM: Glucagon-like peptide-1 receptor agonist (GLP-1RA) therapy is a potential treatment as adjunct to insulin in type 1 diabetes (T1D). However, GLP-1RAs inhibit glucagon secretion and delay gastric emptying (GE) rate and may impair recovery from hypoglycaemia. We evaluated the effect of the GLP-1RA liraglutide on counterregulatory responses and GE rate during hypoglycaemia in persons with T1D. MATERIALS AND METHODS: In a 12-week, randomised, double-blinded, placebo-controlled study, 20 patients aged >18 years with T1D and HbA1c ≥8% (64 mmol/mol) were randomly assigned (1:1) to liraglutide 1...
November 21, 2016: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27863704/cardiovascular-effects-of-glucose-lowering-therapies-for-type-2-diabetes-new-drugs-in-perspective
#15
REVIEW
Peter L Thompson, Timothy M E Davis
PURPOSE: The purpose of this study was to review the results of clinical trials assessing the cardiovascular effects of drugs for type 2 diabetes and the cardiovascular effects of newer available drugs. METHODS: We performed a detailed search of PubMed-listed publications, reports from international meetings, and ongoing studies from clinical trials.gov. FINDINGS: Currently available drugs have neutral or, in some cases, negative effects on cardiovascular outcomes...
November 15, 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/27862902/cardiovascular-events-and-all-cause-mortality-associated-with-sulfonylureas-compared-to-other-antihyperglycaemic-drugs-a-bayesian-meta-analysis-of-survival-data
#16
Steve Bain, Eric Druyts, Chakrapani Balijepalli, Carl A Baxter, Craig Currie, Romita Das, Richard Donnelly, Kamlesh Khunti, Haya Langerman, Paul Leigh, Gaye Siliman, Kristian Thorlund, Kabirraaj Toor, Jiten Vora, Edward J Mills
AIM: Our aim was to conduct a systematic review and meta-analysis to determine the risk of cardiovascular events and all-cause mortality associated with sulfonylureas versus other antihyperglycaemic drugs in patients with type 2 diabetes. MATERIALS AND METHODS: A systematic review of Medline, Embase, Cochrane, and clinicaltrials.gov was conducted comparing sulfonylurea to placebo or other antihyperglycaemic drugs in patients with type 2 diabetes. A cloglog model was employed in the Bayesian framework to obtain comparative hazard ratios between interventions...
November 14, 2016: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27862814/gut-feelings-about-diabetes-and-glp-1-receptor-agonists-lessons-to-be-learnt-from-studies-in-functional-gastrointestinal-disorders
#17
EDITORIAL
Christopher K Rayner, Karen L Jones, Tongzhi Wu, Michael Horowitz
No abstract text is available yet for this article.
November 9, 2016: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27860501/should-glp-1-receptor-agonists-be-the-first-line-of-treatment-for-type-2-diabetes
#18
Richard E Pratley
No abstract text is available yet for this article.
November 2016: Diabetes Technology & Therapeutics
https://www.readbyqxmd.com/read/27860132/occurrence-of-nausea-vomiting-and-diarrhoea-reported-as-adverse-events-in-clinical-trials-studying-glucagon-like-peptide-1-receptor-agonists-a-systematic-analysis-of-published-clinical-trials
#19
Karolin Bettge, Melanie Kahle, Mirna S Abd El Aziz, Juris J Meier, Michael A Nauck
AIM: GLP-1 receptor agonists (RAs) may cause nausea, vomiting or diarrhoea. The purpose was to assess the risk of adverse events (AEs) with GLP-1 RAs and their relation to dose, background medication and duration of action. MATERIAL AND METHODS: The PubMed database was searched and 32 clinical trials with GLP-1 RAs (phase 3) were selected. We performed a systematic analysis and compared the proportion of patients reporting nausea, vomiting or diarrhoea, for different doses and glucose-lowering background medications, and relative to a reference compound within the subclasses of short- (exenatide b...
November 9, 2016: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27859807/putative-tissue-location-and-function-of-the-slc5-family-member-sglt3
#20
Matúš Soták, Joanne Marks, Robert Unwin
Sodium glucose transporter 3 (SGLT3) has attracted interest because of its putative role as a glucose sensor, rather than a sugar transporter, in contrast to its SGLT1 and SGLT2 co-family members. Significant progress has been made in characterizing the electrophysiological properties in vitro of the single human SGLT3 isoform and the two mouse isoforms, SGLT3a and SGLT3b. Although early reports indicated SGLT3 expression in the small intestinal myenteric and submucosal neurones, hypothalamic neurones, portal vein, and kidney, a lack of reliable antibodies has left unanswered its exact tissue and cellular localization...
November 11, 2016: Experimental Physiology
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