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GLP-1 Analogues

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https://www.readbyqxmd.com/read/29130686/thioamide-substitution-selectively-modulates-proteolysis-and-receptor-activity-of-therapeutic-peptide-hormones
#1
Xing Chen, Elizabeth G Mietlicki-Baase, Taylor M Barrett, Lauren E McGrath, Kieran Koch-Laskowski, John J Ferrie, Matthew R Hayes, E James Petersson
Peptide hormones are attractive as injectable therapeutics and imaging agents, but they often require extensive modification by mutagenesis and/or chemical synthesis to prevent rapid in vivo degradation. Alternatively, the single-atom, O-to-S modification of peptide backbone thioamidation has the potential to selectively perturb interactions with proteases while preserving interactions with other proteins, such as target receptors. Here, we use the validated diabetes therapeutic, glucagon-like peptide-1 (GLP-1), and the target of clinical investigation, gastric inhibitory polypeptide (GIP), as proof-of-principle peptides to demonstrate the value of thioamide substitution...
November 13, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29129776/glucagon-like-peptide-1-glp-1-and-neurotransmitters-signaling-in-epilepsy-an-insight-review
#2
REVIEW
Prashant Koshal, Sumit Jamwal, Puneet Kumar
Epilepsy is one of the most prevalent neurological disorder affecting more than 50 million people worldwide. Numerous studies have suggested that an imbalance in glutamatergic (excitatory) and GABAergic (inhibitory) neurotransmitter system is one of the dominating pathophysiological mechanisms underlying the occurrence and progression of seizures. Further, this alteration in GABAergic and glutamatergic system disrupts the delicate balance of other neurotransmitters system in the brain. Emerging strides have documented the protective role of GLP-1 signaling on altered neurotransmitters signaling in Epilepsy and associated co-morbidities...
November 9, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29105987/a-ketone-ester-drink-lowers-human-ghrelin-and-appetite
#3
Brianna J Stubbs, Pete J Cox, Rhys D Evans, Malgorzata Cyranka, Kieran Clarke, Heidi de Wet
OBJECTIVE: The ketones d-β-hydroxybutyrate (BHB) and acetoacetate are elevated during prolonged fasting or during a "ketogenic" diet. Although weight loss on a ketogenic diet may be associated with decreased appetite and altered gut hormone levels, it is unknown whether such changes are caused by elevated blood ketones. This study investigated the effects of an exogenous ketone ester (KE) on appetite. METHODS: Following an overnight fast, subjects with normal weight (n = 15) consumed 1...
November 6, 2017: Obesity
https://www.readbyqxmd.com/read/29105359/glp-1-analogue-exendin-4-modulates-mapks-activity-but-not-the-heat-shock-response-in-human-hepg2-cells
#4
Dhanya Madhu, Maha Hammad, Sina Kavalakatt, Abdelkrim Khadir, Ali Tiss
PURPOSE: Glucagon-like peptide-1 (GLP-1) analogues reduce ER stress and inflammation in key metabolic organs, including the liver. However, their effects on heat shock response (HSR) and mitogen-activated protein kinases (MAPKs) have not yet been elucidated. In the present study, we investigated whether the GLP-1 analogue, exendin-4, triggers the expression of HSR and increases MAPK activity under metabolic stress. EXPERIMENTAL DESIGN: The effects of exendin-4 in the presence or absence of palmitic acid (PA; 400 μM) or glucose (30 mM) in the HepG2 liver cell line were assessed using Western blots, quantitative real-time PCR and label-free proteomics...
November 3, 2017: Proteomics. Clinical Applications
https://www.readbyqxmd.com/read/29095895/exendin-4-a-glucagon-like-peptide-1-analogue-accelerates-healing-of-chronic-gastric-ulcer-in-diabetic-rats
#5
Yen-Cheng Chen, Ching-Chun Ho, Chih-Hsun Yi, Xiu-Zhu Liu, Tzu-Ting Cheng, Chen-Fuh Lam
BACKGROUND: Diabetes mellitus is an independent risk factor for impaired healing of peptic ulcers, and there are currently no supplementary therapeutics other than the standard antipeptic medicine to improve the ulcer healing in diabetes. This study examined the potential pleiotropic effect of a glucagon-like peptide (Glp)-1 analogue exendin (Ex)-4 on the regeneration of gastric ulcer in streptozotocin-induced diabetic rats. METHODS AND RESULTS: Chronic ulcer was created in rat stomach by submucosal injection of acetic acid and peri-ulcer tissues were analyzed 7 days after operation...
2017: PloS One
https://www.readbyqxmd.com/read/29094257/the-effects-of-exendin-4-on-bone-marrow-derived-mesenchymal-cells
#6
Paola Luciani, Benedetta Fibbi, Benedetta Mazzanti, Cristiana Deledda, Lara Ballerini, Alessandra Aldinucci, Susanna Benvenuti, Riccardo Saccardi, Alessandro Peri
PURPOSE: GLP-1 receptor agonists are antidiabetic drugs currently used in the therapy of type 2 diabetes. Despite several in vitro and in vivo animal studies suggesting a beneficial effect of GLP-1 analogues on bone, in humans their skeletal effects are not clear and clinical studies report conflicting results. METHODS: We differentiated human mesenchymal stromal cells (hMSC) toward the adipogenic and the osteoblastic lineages, analysing the effect of Exendin-4 (EXE) before, during and after specific differentiations...
November 1, 2017: Endocrine
https://www.readbyqxmd.com/read/29055668/effect-of-meal-size-and-texture-on-gastric-pouch-emptying-and-glucagon-like-peptide-1-after-gastric-bypass-surgery
#7
Sarah Stano, Fatima Alam, Louis Wu, Roxanne Dutia, Sin-Nee Ng, Margarita Sala, James McGinty, Blandine Laferrère
BACKGROUND: Roux-en-Y gastric bypass (RYGB) accelerates gastric pouch emptying, enhances postprandial glucagon-like peptide 1 (GLP-1) and insulin, and lowers glucose concentrations. To prevent discomfort and reactive hypoglycemia, it is recommended that post-RYGB patients eat small, frequent meals and avoid caloric drinks. However, the effect of meal size and texture on GLP-1 and metabolic response has not been studied. OBJECTIVES: To demonstrate that frequent minimeals and solid meals (S) elicit less GLP-1 and insulin release and less reactive hypoglycemia and are better tolerated compared with a single isocaloric liquid meal (L)...
September 9, 2017: Surgery for Obesity and related Diseases: Official Journal of the American Society for Bariatric Surgery
https://www.readbyqxmd.com/read/29051554/recombinant-incretin-secreting-microbe-improves-metabolic-dysfunction-in-high-fat-diet-fed-rodents
#8
Paul M Ryan, Elaine Patterson, Robert M Kent, Helena Stack, Paula M O'Connor, Kiera Murphy, Veronica L Peterson, Rupasri Mandal, David S Wishart, Timothy G Dinan, John F Cryan, Randy J Seeley, Catherine Stanton, R Paul Ross
The gut hormone glucagon-like peptide (GLP)-1 and its analogues represent a new generation of anti-diabetic drugs, which have also demonstrated propensity to modulate host lipid metabolism. Despite this, drugs of this nature are currently limited to intramuscular administration routes due to intestinal degradation. The aim of this study was to design a recombinant microbial delivery vector for a GLP-1 analogue and assess the efficacy of the therapeutic in improving host glucose, lipid and cholesterol metabolism in diet induced obese rodents...
October 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29044772/rd-lawrence-lecture-2017-incretins-the-intelligent-hormones-in-diabetes
#9
V A Gault
The incretin hormones glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) have attracted considerable scientific and clinical interest due largely to their insulin-releasing and glucose-lowering properties. Indeed, GLP-1-based therapies are now key treatment options for many people with diabetes worldwide. In contrast, GIP-based agents have yet to reach the clinic based primarily on the impaired insulinotropic action of GIP observed in people with diabetes. Nevertheless, GIP is a key physiological regulator of insulin secretion and stable forms of GIP show much promise in rodent models to alleviate diabetes-obesity...
October 16, 2017: Diabetic Medicine: a Journal of the British Diabetic Association
https://www.readbyqxmd.com/read/29042458/exenatide-modulates-tumor-endothelial-cell-interactions-in-human-ovarian-cancer-cells
#10
Agnieszka Kosowska, Enrique Gallego-Colon, Wojciech Garczorz, Agnieszka Kłych-Ratuszny, Mohammad Reza F Aghdam, Michał Woz Niak, Andrzej Witek, Agnieszka Wróblewska-Czech, Anna Cygal, Jerzy Wojnar, Tomasz Francuz
Diabetes and cancer are prevalent diseases whose incidence is increasing globally. Diabetic women have a moderate risk increase in ovarian cancer, suggested to be due to an interaction between these two disorders. Furthermore, patients manifesting both diseases have associated worse prognosis, reduced survival and shorter relapse-free survival. According to current recommendations, incretin drugs such as Exenatide, a synthetic analog of Exendin-4, and Liraglutide are used as therapy for the type 2 diabetes (T2D)...
November 2017: Endocrine Connections
https://www.readbyqxmd.com/read/28981239/-diabetes-care-pathways-and-the-diabetic-convention-in-2017
#11
V de Brouckère, L Plat
Diabetes is a chronic, pandemic disorder which has a growing impact on healthcare costs and leads to severe micro- and macro-vascular complications. In 2009, Belgium introduced " care trajectories " (CT), a program which allows multidisciplinary management of this disease. CT is built on a partnership between three parties: the patient (central to the concept), the general practitioner (GP) and the diabetologist. The GP is responsible for the medical management according to an individualized care plan. The specialist's task is to update the GPs' knowledge and to coach them...
2017: Revue Médicale de Bruxelles
https://www.readbyqxmd.com/read/28948559/effects-of-pegylated-glucagon-like-peptide-1-analogue-in-c57bl-6-mice-under-optimal-conditions-and-during-streptozotocin-induced-diabetes
#12
E G Skurikhin, O V Stronin, A A Epanchintsev, O V Pershina, N N Ermakova, V A Krupin, A V Pakhomova, O E Vaizova, A M Dygai
Biological activity of a new pegylated form of an of glucagon-like peptide-1 (GLP-1) analogue pegGLP-1 was studied in C57Bl/6 mice under normal conditions and during modeling of streptozotocin-induced type I diabetes mellitus. pegGLP-1 differs from GLP-1 (7-37) by polyethylene glycol residue covalently bound to His7, Lys26, and Lys34 of the GLP-1 molecule. It was shown that single intragastrical administration of pegGLP-1 induced an increase in GLP-1 level in blood serum of healthy mice. The maximum level of this parameter was observed in 4-8 h...
September 26, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28947828/fenugreek-compound-n55-lowers-plasma-glucose-through-the-enhancement-of-response-of-physiological-glucagon-like-peptide-1
#13
I-Wen Chou, Yu-Hong Cheng, Yet-Ran Chen, Patrick Ching-Ho Hsieh, Klim King
Glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) analogues are approved for treating type 2 diabetes, but are known to activate GLP-1R signaling globally and constitutively. Active compound N55, previously isolated from fenugreek, enhances the potency of GLP-1 without activating GLP-1R. Here we investigated if N55 lowers plasma glucose base on physiological levels of GLP-1. N55 was found to dose-dependently lower plasma glucose in non-fasted mice but not in the fasted mice, with the effect attenuated by GLP-1R antagonist exendin-(9-39) (Ex-9)...
September 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28919123/liraglutide-a-glucagon-like-peptide-1-receptor-agonist-facilitates-osteogenic-proliferation-and-differentiation-in-mc3t3-e1-cells-through-phosphoinositide-3-kinase-pi3k-protein-kinase-b-akt-extracellular-signal-related-kinase-erk-1-2-and-camp-protein-kinase
#14
Xuelun Wu, Shilun Li, Peng Xue, Yukun Li
Previous studies have proven that glucagon-like peptide-1 (GLP-1) and its receptor agonist exert favorable anabolic effects on skeletal metabolism. However, whether GLP-1 could directly impact osteoblast-mediated bone formation is still controversial, and the underlying molecular mechanism remains to be elucidated. Thus in this paper, we investigated the effects of liraglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist, on murine MC3T3-E1 preosteoblasts proliferation and differentiation and explored the potential cellular basis...
November 15, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28864549/atrial-natriuretic-peptide-anp-affects-stimulus-secretion-coupling-of-pancreatic-%C3%AE-cells
#15
Sabrina Undank, Julia Kaiser, Jelena Sikimic, Martina Düfer, Peter Krippeit-Drews, Gisela Drews
ANP influences glucose homeostasis and possibly acts as a link between the cardiovascular system and metabolism, especially in metabolic disorders like diabetes. The present study aimed to evaluate effects of ANP on β-cell function by the use of a β-cell specific knockout of the ANP receptor with guanylate cyclase activity (βGC-A-KO). ANP augmented insulin secretion at the threshold glucose concentration of 6 mM and decreased KATP single channel activity in β-cells of control mice but not of βGC-A-KO mice...
September 1, 2017: Diabetes
https://www.readbyqxmd.com/read/28846606/the-emerging-role-of-glp-1-receptors-in-dna-repair-implications-in-neurological-disorders
#16
REVIEW
Jenq-Lin Yang, Wei-Yu Chen, Shang-Der Chen
Glucagon-like peptide-1 (GLP-1) is originally found as a metabolic hormone (incretin) that is able to regulate blood-glucose levels via promoting synthesis and secretion of insulin. GLP-1 and many analogues are approved for treatment of type II diabetes. Accumulating results imply that GLP-1 performs multiple functions in various tissues and organs beyond regulation of blood-glucose. The neuroprotective function of GLP-1 has been extensively explored during the past two decades. Three of our previous studies have shown that apurinic/apyrimidinic endonuclease 1 (APE1) is the only protein of the base excision repair (BER) pathway able to be regulated by oxidative stress or exogenous stimulations in rat primary cortical neurons...
August 26, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28836148/anti-diabetic-actions-of-esculentin-2cha-1-30-and-its-stable-analogues-in-a-diet-induced-model-of-obesity-diabetes
#17
Srividya Vasu, Opeolu O Ojo, R Charlotte Moffett, J Michael Conlon, Peter R Flatt, Yasser H A Abdel-Wahab
Actions of esculentin-2CHa(1-30) (GFSSIFRGVAKFASKGLGKDLAKLGVDLVA) and its analogues, ([D-Arg(7), D-Lys(15), D-Lys(23)]-esculentin-2CHa(1-30) and [Lys(15)-octanoate]-esculentin-2CHa(1-30), were evaluated in high-fat fed NIH Swiss mice with impaired glucose tolerance and insulin resistance. Twice-daily i.p. administration of the esculentin-2CHa(1-30) peptides (75 nmol/kg body weight) or exendin-4 (25 nmol/kg) for 28 days reduced body weight, without altering cumulative energy intake. All peptides reduced blood glucose levels by 6-12 mmol/l concomitant with lower plasma insulin levels, with significance evident from day 6...
October 2017: Amino Acids
https://www.readbyqxmd.com/read/28831150/glp-1-exendin-4-induces-%C3%AE-cell-proliferation-via-the-epidermal-growth-factor-receptor
#18
Joseph Fusco, Xiangwei Xiao, Krishna Prasadan, Qingfeng Sheng, Congde Chen, Yung-Ching Ming, George Gittes
Exendin-4 is a long acting glucagon-like peptide 1 (GLP-1) analogue that is an agonist for the GLP-1 receptor, a G-protein coupled receptor (GPCR). Exendin-4 is used to clinically improve glucose tolerance in diabetic patients due to its ability to enhance insulin secretion. In rodents, and possibly in humans, exendin-4 can stimulate β-cell proliferation. The exact mechanism of action to induce β-cell proliferation is not well understood. Here, using a β-cell specific epidermal growth factor receptor (EGFR) null mouse, we show that exendin-4 induced an increase in proliferation and β-cell mass through EGFR...
August 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28808865/glucagon-like-peptides-1-and-2-are-involved-in-satiety-modulation-after-modified-biliopancreatic-diversion-results-of-a-pilot-study
#19
Everton Cazzo, José Carlos Pareja, Elinton Adami Chaim, Cláudio Saddy Rodrigues Coy, Daniéla Oliveira Magro
BACKGROUND: This paper aimed to evaluate the influence of modified biliopancreatic diversion (BPD) on the levels of GLP-1 and GLP-2 and correlate them with satiety regulation. METHODS: This is a pilot prospective cohort study that evaluated six mildly obese individuals with type 2 diabetes mellitus, which underwent modified BPD and were followed-up for 12 months. Levels of GLP-1 and GLP-2 after a standard meal tolerance test were determined and correlated with satiety scores obtained by means of a visual analogue scale (VAS)...
August 14, 2017: Obesity Surgery
https://www.readbyqxmd.com/read/28772236/a-novel-glucagon-like-peptide-1-glucagon-receptor-dual-agonist-exhibits-weight-lowering-and-diabetes-protective-effects
#20
Jie Zhou, Xingguang Cai, Xun Huang, Yuxuan Dai, Lidan Sun, Bo Zhang, Bo Yang, Haiyan Lin, Wenlong Huang, Hai Qian
Glucagon has plenty of effects via a specific glucagon receptor(GCGR) like elevating the blood glucose, improving fatty acids metabolism, energy expenditure and increasing lipolysis in adipose tissue. The most important role of glucagon is to regulate the blood glucose, but the emergent possibilities of hyperglycaemia is exist. Glucagon could also slightly activate glucagon-like peptide-1 receptor(GLP-1R), which lead to blood glucose lowering effect. This study aims to erase the likelihood of hyperglycaemia and to remain the inherent catabolic effects through improving GLP-1R activation and deteriorating GCGR activation so as to lower the bodyweight and show diabetes-protective effects...
September 29, 2017: European Journal of Medicinal Chemistry
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