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GLP-1 Analogues

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https://www.readbyqxmd.com/read/28323117/absorption-metabolism-and-excretion-of-the-glp-1-analogue-semaglutide-in-humans-and-nonclinical-species
#1
Lene Jensen, Hans Helleberg, Ad Roffel, Jan Jaap van Lier, Inga Bjørnsdottir, Palle Jacob Pedersen, Everton Rowe, Julie Derving Karsbøl, Mette Lund Pedersen
Semaglutide is a human glucagon-like peptide-1 analogue in clinical development for the treatment of type 2 diabetes. The absorption, metabolism and excretion of a single 0.5mg/450μCi [16.7MBq] subcutaneous dose of [(3)H]-radiolabelled semaglutide was investigated in healthy human subjects and compared with data from nonclinical studies. Radioactivity in blood, plasma, urine and faeces was determined in humans, rats and monkeys; radioactivity in expired air was determined in humans and rats. Metabolites in plasma, urine and faeces were quantified following profiling and radiodetection...
March 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28315374/glp-1-analogue-cjc-1131-prevents-amyloid-%C3%AE-protein-induced-impirments-of-spatial-memory-and-synaptic-plasticity-in-rats
#2
Sheng-Xiao Zhang, Hong-Yan Cai, Xiao-Wen Ma, Li Yuan, Jun Zhang, Zhao-Jun Wang, Yu-Feng Li, Jin-Shun Qi
Although amyloid β protein (Aβ) has been recognized as one of the main pathological characteristics in the brain of Alzheimer's disease (AD), the effective strategies against Aβ neurotoxicity are still deficient up to now. Glucagon-like peptide 1 (GLP-1), a natural gut hormone, was found to be effective in modulating insulin signaling and neural protection, but short half-life limited its clinical application in AD treatment. CJC-1131, a newly designed GLP-1 analogue with very longer half-life, has shown good effectiveness in the treatment of type 2 diabetes mellitus (T2DM)...
March 14, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28292761/optimization-of-tolerability-and-efficacy-of-dual-amylin-and-calcitonin-receptor-agonist-kbp-089-through-dose-escalation-and-combination-with-a-glp-1-analogue
#3
Sofie Gydesen, Kim Vietz Andreassen, Sara Toftegaard Hjuler, Lars I Hellgren, Morten Asser Karsdal, Kim Henriksen
Amylin and GLP-1 agonism induce a well-known anorexic effect at dose initiation, which is managed by dose escalation. In this study, we investigated how to optimize tolerability, while maintaining efficacy of KBP-089. Furthermore, we tested the GLP-1 add-on potential of KBP-089 in HFD rats. KBP-089 potently activated both the amylin and calcitonin receptors in vitro, demonstrated a prolonged receptor activation, and potently reduced acute food intake. HFD rats dosed every or every second day obtained equal weight loss at study end, albeit with an uneven reduction in both food intake and bodyweight in rats dosed every second day...
March 14, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28286674/the-effect-of-exercise-intensity-on-total-pyy-and-glp-1-in-healthy-females-a-pilot-study
#4
Jillian R Hallworth, Jennifer L Copeland, Jon Doan, Tom J Hazell
We compared the acute response of anorexigenic signals (total PYY and GLP-1) in response to submaximal and supramaximal exercise. Nine females completed three sessions: (1) moderate-intensity continuous training (MICT; 30 min; 65%  VO2max); (2) sprint interval training (SIT; 6 × 30 sec "all-out" cycling sprints with 4 min recovery); or (3) control (CTRL; no exercise). PYY and GLP-1 were measured via blood samples drawn before, immediately after, and 90 min after exercise. Perceptions of hunger were rated using a visual analogue scale at all blood sampling time points...
2017: Journal of Nutrition and Metabolism
https://www.readbyqxmd.com/read/28245771/current-drug-targets-in-obesity-pharmacotherapy-a-review
#5
Sangeeta P Bhat, Arun Sharma
Obesity, an impending global pandemic, is not being effectively controlled by current measures such as lifestyle modifications, bariatric surgery or available medications. Its toll on health and economy compels us to look for more effective measures. Fortunately, the advances in biology and molecular technology have been in our favour for delineating new pathways in the pathophysiology of obesity and have led to subsequent development of new drug targets. Development of anti-obesity drugs has often been riddled with problems in the past...
February 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28242257/exendin-4-inhibits-structural-remodeling-and-improves-ca-2-homeostasis-in-rats-with-heart-failure-via-the-glp-1-receptor-through-the-enos-cgmp-pkg-pathway
#6
Jingjing Chen, Dandan Wang, Fangai Wang, Shaobo Shi, Yuting Chen, Bo Yang, Yanhong Tang, Congxin Huang
The glucagon-like peptide-1 receptor (GLP-1R) agonist exendin-4 is a long-acting analog of GLP-1, which stimulates insulin secretion and is clinically used in the treatment of type 2 diabetes. Previous studies have demonstrated that GLP-1 agonists and analogs serve as cardioprotective factors in various conditions. Disturbances in calcium cycling are characteristic of heart failure (HF); therefore, the aim of this study was to investigate the effect of exendin-4 (a GLP-1 mimetic) on the regulation of calcium handling and to identify the underlying mechanisms in an HF rat model after myocardial infarction (MI)...
February 24, 2017: Peptides
https://www.readbyqxmd.com/read/28237265/treating-prediabetes-in-the-obese-are-glp-1-analogues-the-answer
#7
Olivia M Farr, Christos S Mantzoros
No abstract text is available yet for this article.
February 22, 2017: Lancet
https://www.readbyqxmd.com/read/28223210/a-novel-glp-1-gip-dual-receptor-agonist-protects-from-6-ohda-lesion-in-a-rat-model-of-parkinson-s-disease
#8
Jaishree Jalewa, Mohit Kumar Sharma, Simon Gengler, Christian Hölscher
The incretins glucagon-like peptide 1 (GLP-1) and glucose dependent insulinotropic polypeptide (GIP) are growth factors that have shown neuroprotective effects in animal models of Parkinson's and Alzheimer's disease. In addition, the GLP-1 mimetic exendin-4 has shown protective effects in a clinical trial in Parkinson's disease (PD) patients. GLP-1 analogues are currently on the market as treatments for type II diabetes. We previously showed that the novel dual agonist (DA-JC1) was effective in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of PD...
February 20, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28222742/resistant-starch-lowers-postprandial-glucose-and-leptin-in-overweight-adults-consuming-a-moderate-to-high-fat-diet-a-randomized-controlled-trial
#9
Mindy Patterson Maziarz, Sara Preisendanz, Shanil Juma, Victorine Imrhan, Chandan Prasad, Parakat Vijayagopal
BACKGROUND: High-amylose maize resistant starch type 2 (HAM-RS2) stimulates gut-derived satiety peptides and reduces adiposity in animals. Human studies have not supported these findings despite improvements in glucose homeostasis and insulin sensitivity after HAM-RS2 intake which can lower adiposity-related disease risk. The primary objective of this study was to evaluate the impact of HAM-RS2 consumption on blood glucose homeostasis in overweight, healthy adults. We also examined changes in biomarkers of satiety (glucagon-like peptide-1 [GLP-1], peptide YY [PYY], and leptin) and body composition determined by anthropometrics and dual-energy x-ray absorptiometry, dietary intake, and subjective satiety measured by a visual analogue scale following HAM-RS2 consumption...
February 21, 2017: Nutrition Journal
https://www.readbyqxmd.com/read/28222044/endocrine-system-on-chip-for-a-diabetes-treatment-model
#10
Dao Thi Thuy Nguyen, Danny van Noort, In-Kyung Jeong, Sungsu Park
The endocrine system is a collection of glands producing hormones which, among others, regulates metabolism, growth and development. One important group of endocrine diseases is diabetes, which is caused by a deficiency or diminished effectiveness of endogenous insulin. By using a microfluidic perfused 3D cell-culture chip, we developed an 'endocrine system on chip' to potentially be able to screen drugs for the treatment of diabetes by measuring insulin release over time. Insulin-secreting β-cells are located in the pancreas, while L-cells, located in the small intestines, stimulate insulin secretion...
February 21, 2017: Biofabrication
https://www.readbyqxmd.com/read/28216550/the-acute-effects-of-simple-sugar-ingestion-on-appetite-gut-derived-hormone-response-and-metabolic-markers-in-men
#11
Adora M W Yau, John McLaughlin, William Gilmore, Ronald J Maughan, Gethin H Evans
This pilot study aimed to investigate the effect of simple sugar ingestion, in amounts typical of common ingestion, on appetite and the gut-derived hormone response. Seven healthy men ingested water (W) and equicaloric solutions containing 39.6 g glucose monohydrate (G), 36 g fructose (F), 36 g sucrose (S), and 19.8 g glucose monohydrate + 18 g fructose (C), in a randomised order. Serum concentrations of ghrelin, glucose dependent insulinotropic polypeptide (GIP), glucagon like peptide-1 (GLP-1), insulin, lactate, triglycerides, non-esterified fatty acids (NEFA), and d-3 hydroxybutyrate, were measured for 60 min...
February 14, 2017: Nutrients
https://www.readbyqxmd.com/read/28209419/a-safety-and-pharmacokinetic-dosing-study-of-glucagon-like-peptide-2-in-infants-with-intestinal-failure
#12
David L Sigalet, Mary E Brindle, Dana Boctor, Bryan Dicken, Viona Lam, Lily Sia Lu, Elaine de Heuvel, Bolette Hartmann, Jens J Holst
BACKGROUND & AIMS: Glucagon-like peptide 2 (GLP-2) analogues are approved for adults with intestinal failure (IF), but no studies have included infants. This study examined the pharmacokinetics (PK), safety, and nutritional effects of GLP-2 in infants with IF. METHODS: With parental consent (Health Canada Protocol:150,979), parenteral nutrition (PN)-dependent infants were treated with 5-20-μg/kg/day GLP-2 for 3days (phase 1), and if tolerated continued for 42days (phase 2)...
January 29, 2017: Journal of Pediatric Surgery
https://www.readbyqxmd.com/read/28204823/incretins-amplify-tnf-%C3%AE-stimulated-il-6-synthesis-in-osteoblasts-suppression-of-the-i%C3%AE%C2%BAb-nf-%C3%AE%C2%BAb-pathway
#13
Kazuhiko Fujita, Haruhiko Tokuda, Naohiro Yamamoto, Shingo Kainuma, Tetsu Kawabata, Go Sakai, Gen Kuroyanagi, Rie Matsushima-Nishiwaki, Atsushi Harada, Osamu Kozawa, Takanobu Otsuka
Incretins including glucagon-like peptide-1 (GLP-1) and glucose‑dependent insulinotropic polypeptide (GIP) secreted from the small intestine after oral food ingestion are currently recognized to stimulate insulin secretion from pancreatic β cells. We previously reported that p70 S6 kinase limits the tumor necrosis factor‑α (TNF‑α)‑stimulated interleukin-6 (IL‑6) synthesis in osteoblast‑like MC3T3‑E1 cells. In the present study, we investigated the effects of incretins on the TNF‑α‑induced IL‑6 synthesis and the underlying mechanism in MC3T3‑E1 cells...
February 15, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28161303/comparison-of-exenatide-and-acarbose-on-intra-abdominal-fat-content-in-patients-with-obesity-and-type-2-diabetes-a-randomized-controlled-trial
#14
Li Shi, Jing Zhu, Ping Yang, Xiaoqiang Tang, Wenlong Yu, Changjie Pan, Moyu Shen, Dalong Zhu, Jinluo Cheng, Xinhua Ye
OBJECTIVE: To investigate exenatide, a GLP-1 analogue, compared with acarbose, for intra-abdominal fat reduction in patients with obesity and type-2 diabetes. METHODS: This randomized controlled trial included 36 patients with obesity and type-2 diabetes, who were metformin-unresponsive, receiving metformin/exenatide (GLP-1 group) or metformin/acarbose (control group) for 3 months. Primary end-point: intra-abdominal fat content from baseline to 3 months; Secondary end-points: changes in fasting blood glucose, glycated haemoglobin (HbAlc), fasting insulin, blood lipids, weight, body mass index, and inflammatory cytokines from baseline to 3 months...
February 1, 2017: Obesity Research & Clinical Practice
https://www.readbyqxmd.com/read/28154977/sex-differences-in-the-response-of-total-pyy-and-glp-1-to-moderate-intensity-continuous-and-sprint-interval-cycling-exercise
#15
Tom J Hazell, Logan K Townsend, Jillian R Hallworth, Jon Doan, Jennifer L Copeland
BACKGROUND: Exercise interventions are often less effective at improving body composition for females than males, potentially due to post-exercise hormonal responses that increase energy intake in females. Recently, sprint interval training was shown to effectively reduce body fat in females despite being relatively low during exercise energy expenditure. PURPOSE: To determine whether any sex difference in total PYY, GLP-1 or perceived hunger exists following moderate-intensity continuous exercise (MICT) and sprint interval exercise (SIT) METHODS: Twenty-one active participants (11 females) participated in three sessions in a randomized crossover design: (1) MICT, 30-min cycling at 65% VO2max; (2) SIT, 6 × 30 s "all-out" sprints with 4-min recovery periods; (3) control (CTRL; no exercise)...
March 2017: European Journal of Applied Physiology
https://www.readbyqxmd.com/read/28152036/bioactivity-of-a-modified-human-glucagon-like-peptide-1
#16
Fangfang Xu, Kevin Yueju Wang, Nan Wang, Gangqiang Li, Dehu Liu
Diabetes has become the third largest cause of death in humans worldwide. Therefore, effective treatment for this disease remains a critical issue. Glucagon-like peptide-1 (GLP-1) plays an important role in glucose homeostasis, and therefore represents a promising candidate to use for the treatment of diabetes. Native GLP-1, however, is quickly degraded in in the circulatory system; which limits its clinical application. In the present study, a chemically-synthesized, modified analogue of human GLP-1 (mGLP-1) was designed...
2017: PloS One
https://www.readbyqxmd.com/read/28145471/synergistic-effects-of-metformin-with-liraglutide-against-endothelial-dysfunction-through-glp-1-receptor-and-pka-signalling-pathway
#17
Jing Ke, Ye Liu, Jin Yang, Ran Lu, Qing Tian, Wenfang Hou, Guang Wang, Rui Wei, Tianpei Hong
Metformin or glucagon-like peptide-1 (GLP-1) analogue liraglutide has cardiovascular benefits. However, it is not clear whether their combined treatment have additive or synergistic effects on the vasculature. In this study, human umbilical vein endothelial cells (HUVECs), exposed to palmitic acid (PA) to induce endothelial dysfunction, were incubated with metformin, liraglutide or their combination. High fat diet (HFD)-fed ApoE(-/-) mice were randomized into control, metformin, liraglutide, and combination treatment groups...
February 1, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28127745/5-fluorouracil-causes-endothelial-cell-senescence-potential-protective-role-of-glucagon-like-peptide-1
#18
Paola Altieri, Roberto Murialdo, Chiara Barisione, Edoardo Lazzarini, Silvano Garibaldi, Patrizia Fabbi, Clarissa Ruggeri, Silvia Borile, Federico Carbone, Andrea Armirotti, Marco Canepa, Alberto Ballestrero, Claudio Brunelli, Fabrizio Montecucco, Pietro Ameri, Paolo Spallarossa
BACKGROUND AND PURPOSE: 5-fluorouracil (5FU) and its prodrug, capecitabine, can damage endothelial cells, whilst endothelial integrity is preserved by glucagon-like peptide 1 (GLP-1). Here, we studied the effect of 5FU on endothelial senescence and whether GLP-1 antagonizes it. EXPERIMENTAL APPROACH: EA.hy926 cells were exposed to 5FU or sera from patients taking capecitabine, with or without pre-incubation with GLP-1. Senescence was identified by expression of senescence-associated β-galactosidase and p16(INK4a) and reduced cell proliferation...
January 27, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28115493/esculentin-2cha-1-30-and-its-analogues-stability-and-mechanisms-of-insulinotropic-action
#19
Srividya Vasu, Mary K McGahon, R Charlotte Moffett, Tim M Curtis, J Michael Conlon, Yasser H A Abdel-Wahab, Peter R Flatt
The insulin-releasing effects, cellular mechanisms of action and anti-hyperglycaemic activity of 10 analogues of esculentin-2CHa lacking the cyclic C-terminal domain (CKISKQC) were evaluated. Analogues of the truncated peptide, esculentin-2CHa(1-30), were designed for plasma enzyme resistance and increased biological activity. Effects of those analogues on insulin release, cell membrane integrity, membrane potential, intracellular Ca(2+) and cAMP levels were determined using clonal BRIN-BD11 cells. Their acute effects on glucose tolerance were investigated using NIH Swiss mice...
March 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/28110911/efficacy-and-safety-of-once-weekly-semaglutide-monotherapy-versus-placebo-in-patients-with-type-2-diabetes-sustain-1-a-double-blind-randomised-placebo-controlled-parallel-group-multinational-multicentre-phase-3a-trial
#20
Christopher Sorli, Shin-Ichi Harashima, George M Tsoukas, Jeffrey Unger, Julie Derving Karsbøl, Thomas Hansen, Stephen C Bain
BACKGROUND: Despite a broad range of pharmacological options for the treatment of type 2 diabetes, optimum glycaemic control remains challenging for many patients and new therapies are necessary. Semaglutide is a glucagon-like peptide-1 (GLP-1) analogue in phase 3 development for type 2 diabetes. We assessed the efficacy, safety, and tolerability of semaglutide monotherapy, compared with placebo, in treatment-naive patients with type 2 diabetes who had insufficient glycaemic control with diet and exercise alone...
January 16, 2017: Lancet Diabetes & Endocrinology
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