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https://www.readbyqxmd.com/read/29673717/novel-fatty-acid-chain-modified-glp-1-derivatives-with-prolonged-in-vivo-glucose-lowering-ability-and-balanced-glucoregulatory-activity
#1
Xingguang Cai, Lidan Sun, Yuxuan Dai, Yosefa Avraham, Chunxia Liu, Jing Han, Yuan Liu, Dazhi Feng, Wenlong Huang, Hai Qian
Glucagon-like peptide-1 is a potent hypoglycemic hormone with beneficial properties for the treatment of diabetes. However, its half-life is short because the rapid metabolic degradation. This study aims to prolong the half-life of glucagon-like peptide-1 through conjugation with the fatty acid side chain which helps the conjugates to interact with the albumin. Firstly, we chose two optimized polypeptide chains which have tremendous hypoglycemic effect named Cys17 -Gly8 -GLP-1(7-36)-NH2 and Cys37 -Gly8 -GLP-1(7-37)-NH2 , and various fatty acid chains were modified...
April 11, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29656185/exogenous-serp1-attenuates-restenosis-by-restoring-glp-1-receptor-activity-in-diabetic-rats-following-vascular-injury
#2
Lishuai Feng, Jianbo Wang, Xu Ma
The activity of glucagon-like peptide 1 (GLP-1R) is essential for preventing restenosis following vascular injury; however, the mechanism of dysfunctional GLP-1R glycosylation and ways to enhance the activity of GLP-1R on vascular surfaces in diabetic patients are poorly understood. In the present study, we investigated the N-glycosylation level and role of stress-associated endoplasmic reticulum protein 1 (SERP1) in preventing restenosis following carotid injury in diabetic rats. Our results showed that N-glycosylation levels in both rat aortic endothelial cells (RAOECs) and rat vascular smooth muscle cells (VSMCs) decreased gradually following glucose treatment in a concentration dependant manner...
April 12, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29650350/loss-of-dorsomedial-hypothalamic-glp-1-signaling-reduces-bat-thermogenesis-and-increases-adiposity
#3
Shin J Lee, Graciela Sanchez-Watts, Jean-Philippe Krieger, Angelica Pignalosa, Puck N Norell, Alyssa Cortella, Klaus G Pettersen, Dubravka Vrdoljak, Matthew R Hayes, Scott Kanoski, Wolfgang Langhans, Alan G Watts
OBJECTIVE: Glucagon-like peptide-1 (GLP-1) neurons in the hindbrain densely innervate the dorsomedial hypothalamus (DMH), a nucleus strongly implicated in body weight regulation and the sympathetic control of brown adipose tissue (BAT) thermogenesis. Therefore, DMH GLP-1 receptors (GLP-1R) are well placed to regulate energy balance by controlling sympathetic outflow and BAT function. METHODS: We investigate this possibility in adult male rats by using direct administration of GLP-1 (0...
March 21, 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29626654/geniposide-improves-repeated-restraint-stress-induced-depression-like-behavior-in-mice-by-ameliorating-neuronal-apoptosis-via-regulating-glp-1r-akt-signaling-pathway
#4
Yinghua Zhao, Hongyan Li, Fang Fang, Tingting Qin, Wei Xiao, Zhenzhong Wang, Shiping Ma
Geniposide (GP), a bioactive iridoid glycoside isolated from Gardenia jasminoides Ellis, as well as an agonist of Glucagon-like peptide-1 receptor (GLP-1R), has been reported to exhibit antidepressant-like effects in several rodent models. However, the underlying mechanisms remain obscure. In this study, we mainly investigated the antidepressant-like effects of GP and explored the possible mechanisms associated with GLP-1R signaling by using the repeated restraint stress (RRS)-induced depression model of mice...
April 4, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29617641/mechanisms-of-action-and-therapeutic-application-of-glucagon-like-peptide-1
#5
REVIEW
Daniel J Drucker
Glucagon-like peptide-1 (GLP-1) released from gut enteroendocrine cells controls meal-related glycemic excursions through augmentation of insulin and inhibition of glucagon secretion. GLP-1 also inhibits gastric emptying and food intake, actions maximizing nutrient absorption while limiting weight gain. Here I review the circuits engaged by endogenous versus pharmacological GLP-1 action, highlighting key GLP-1 receptor (GLP-1R)-positive cell types and pathways transducing metabolic and non-glycemic GLP-1 signals...
April 3, 2018: Cell Metabolism
https://www.readbyqxmd.com/read/29607314/glucagon-like-peptide-1-mediates-the-protective-effect-of-the-dipeptidyl-peptidase-iv-inhibitor-on-renal-fibrosis-via-reducing-the-phenotypic-conversion-of-renal-microvascular-cells-in-monocrotaline-treated-rats
#6
Jian Xu, Jingjing Wang, Yusheng Cheng, Xiang Li, Mengyu He, Jiali Zhu, Honghao Han, Guihong Wei, Hui Kong, Weiping Xie, Hong Wang, Xiangrong Zuo
Chronic kidney diseases are characterized by renal fibrosis with excessive matrix deposition, leading to a progressive loss of functional renal parenchyma and, eventually, renal failure. Renal microcirculation lesions, including the phenotypic conversion of vascular cells, contribute to renal fibrosis. Here, renal microcirculation lesions were established with monocrotaline (MCT, 60 mg/kg). Sitagliptin (40 mg/kg/d), a classical dipeptidyl peptidase-4 (DPP-4) inhibitor, attenuated the renal microcirculation lesions by inhibiting glomerular tuft hypertrophy, glomerular mesangial expansion, and microvascular thrombosis...
2018: BioMed Research International
https://www.readbyqxmd.com/read/29590132/glp-1-receptor-agonist-ameliorates-obesity-induced-chronic-kidney-injury-via-restoring-renal-metabolism-homeostasis
#7
Chengshi Wang, Ling Li, Shuyun Liu, Guangneng Liao, Lan Li, Younan Chen, Jingqiu Cheng, Yanrong Lu, Jingping Liu
Increasing evidence indicates that obesity is highly associated with chronic kidney disease (CKD). GLP-1 receptor (GLP-1R) agonist has shown benefits on kidney diseases, but its direct role on kidney metabolism in obesity is still not clear. This study aims to investigate the protection and metabolic modulation role of liraglutide (Lira) on kidney of obesity. Rats were induced obese by high-fat diet (HFD), and renal function and metabolism changes were evaluated by metabolomic, biological and histological methods...
2018: PloS One
https://www.readbyqxmd.com/read/29545266/native-oxyntomodulin-has-significant-glucoregulatory-effects-independent-of-weight-loss-in-obese-humans-with-and-without-type-2-diabetes
#8
Sudha S Shankar, R Ravi Shankar, Lori A Mixson, Deborah L Miller, Barnali Pramanik, Amy K O'Dowd, Donna M Williams, Clay B Frederick, Chan R Beals, S Aubrey Stoch, Helmut O Steinberg, David E Kelley
Oxyntomodulin (OXM), an enteroendocrine hormone, causes appetite suppression, increased energy expenditure, and weight loss in obese humans via activation of GLP-1 and glucagon receptors. However, the effects of OXM on glucose homeostasis remain ill-defined. To address this gap, we evaluated the effects of an intravenous (IV) infusion of native OXM on insulin secretory rates (ISR) and glycemic excursion in a graded glucose infusion (GGI) procedure in two separate randomized, placebo-controlled, single dose crossover trials in 12 overweight and obese subjects without diabetes, and in 12 obese subjects with Type 2 diabetes (T2DM) respectively, using the GLP-1 analog, liraglutide as a comparator in the T2DM...
March 15, 2018: Diabetes
https://www.readbyqxmd.com/read/29533738/intragastric-nutrient-infusion-reduces-motivation-for-food-in-male-and-female-rats
#9
Calyn B Maske, Gregory C Loney, Nicole Lilly, Sarah J Terrill, Diana L Williams
The idea that gut-derived satiation signals influence food reward has recently gained traction, but this hypothesis is largely based on studies focused on neural circuitry, not the peripherally released signals. Here, we directly tested the hypothesis that intragastric (IG) nutrient infusion can suppress motivation for food. In a series of experiments, IG sucrose infusion (15 kcal) significantly and reliably reduced operant responding for a sucrose reward on a progressive ratio (PR) schedule. Moreover, food deprivation for 24 h before the test session did not prevent the suppressive effect of nutrients...
March 13, 2018: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29532016/conditional-and-reversible-activation-of-class-a-and-b-g-protein-coupled-receptors-using-tethered-pharmacology
#10
Tom Podewin, Julia Ast, Johannes Broichhagen, Nicholas H F Fine, Daniela Nasteska, Philipp Leippe, Manuel Gailer, Teresa Buenaventura, Nisha Kanda, Ben J Jones, Celine M'Kadmi, Jean-Louis Baneres, Jacky Marie, Alejandra Tomas, Dirk Trauner, Anja Hoffmann-Röder, David J Hodson
Understanding the activation and internalization of G protein-coupled receptors (GPCRs) using conditional approaches is paramount to developing new therapeutic strategies. Here, we describe the design, synthesis, and testing of ExONatide , a benzylguanine-linked peptide agonist of the glucagon-like peptide-1 receptor (GLP-1R), a class B GPCR required for maintenance of glucose levels in humans. ExONatide covalently binds to SNAP-tagged GLP-1R-expressing cells, leading to prolonged cAMP generation, Ca2+ rises, and intracellular retention of the receptor...
February 28, 2018: ACS Central Science
https://www.readbyqxmd.com/read/29530599/the-glucagon-like-peptide-1-glp-1-analog-liraglutide-attenuates-renal-fibrosis
#11
Ya-Kun Li, Dong-Xia Ma, Zhi-Min Wang, Xiao-Fan Hu, Shang-Lin Li, Hong-Zhe Tian, Meng-Jun Wang, Yan-Wen Shu, Jun Yang
Renal fibrosis is recognized as the common route of all chronic kidney disease (CKD) progressing to end-stage renal disease (ESRD). Additionally, accumulating evidence suggests that epithelial-mesenchymal transition (EMT) plays a significant role in the process of renal fibrogenesis. Liraglutide is a long-acting glucagon-like peptide-1 (GLP-1) analog that has been widely used to treat type 2 diabetes. Recent studies have demonstrated that the GLP-1 analogs could also exert protective effects in cardiac fibrosis models...
March 9, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29525225/durability-of-protective-effect-of-dulaglutide-on-pancreatic-%C3%AE-cells-in-diabetic-mice-glp-1-receptor-expression-is-not-reduced-despite-long-term-dulaglutide-exposure
#12
T Kimura, A Obata, M Shimoda, H Hirukawa, Y Kanda-Kimura, Y Nogami, K Kohara, S Nakanishi, T Mune, K Kaku, H Kaneto
AIMS: It is well-known that chronic exposure to large amounts of ligand leads to downregulation of its receptor. It is not known, however, whether a GLP-1R agonist downregulates its receptor. For this reason, our study examined whether GLP-1R expression is reduced after long-term exposure to dulaglutide (Dula) in non-diabetic and diabetic mice. METHODS: Seven-week-old male db/db and db/m mice were given either Dula (0.6mg/kg×2/week) or a control vehicle (CTL) for 17 weeks...
February 6, 2018: Diabetes & Metabolism
https://www.readbyqxmd.com/read/29524296/liraglutide-a-human-glucagon-like-peptide-1-analogue-stimulates-akt-dependent-survival-signalling-and-inhibits-pancreatic-%C3%AE-cell-apoptosis
#13
Katerina Kapodistria, Effie-Photini Tsilibary, Eleni Kotsopoulou, Petros Moustardas, Paraskevi Kitsiou
Liraglutide, a human long-lasting GLP-1 analogue, is currently regarded as a powerful treatment option for type 2 diabetes. Apart from glucoregulatory and insulinotropic actions, liraglutide increases β-cell mass through stimulation of β-cell proliferation and islet neogenesis, as well as inhibition of β-cell apoptosis. However, the underline molecular mechanisms have not been fully characterized. In this study, we investigated the mechanism by which liraglutide preserves islet β-cells in an animal model of overt diabetes, the obese db/db mice, and protects a mouse pancreatic β-cell line (βTC-6 cells) against apoptosis...
March 10, 2018: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29523188/azoramide-a-novel-regulator-favors-adipogenesis-against-osteogenesis-through-inhibiting-the-glp-1-receptor-pka-%C3%AE-catenin-pathway
#14
Banjun Ruan, Zheng Zhu, Zhao Yan, Wei Yang, Dongsheng Zhai, Li Wang, Zichen Ye, Huanyu Lu, An Xiang, Jingwei Liang, Yinghao Jiang, Chengming Xu, Zhenyu Wang, Ming Wei, Xiaoying Lei, Xiaorui Cao, Zifan Lu
BACKGROUND: The reciprocal fate decision of mesenchymal stem cells (MSCs) to either bone or adipocytes is determined by Wnt-related signaling and the glucagon-like peptide-1 receptor (GLP-1R). Azoramide, an ER stress alleviator, was reported to have an antidiabetic effect. In this study, we investigated the function of azoramide in regulating the lineage determination of MSCs for either adipogenic or osteogenic differentiation. METHODS: In this study, microcomputed tomography and histological analysis on bone morphogenetic protein (BMP)2-induced parietal periosteum bone formation assays, C3H10T1/2 and mouse bone marrow MSC-derived bone formation and adipogenesis assays, and specific staining for bone tissue and lipid droplets were used to evaluate the role of azoramide on the lineage determination of MSC differentiation...
March 9, 2018: Stem Cell Research & Therapy
https://www.readbyqxmd.com/read/29510158/endogenous-glp-1-in-lateral-septum-contributes-to-stress-induced-hypophagia
#15
Sarah J Terrill, Calyn B Maske, Diana L Williams
Glucagon-like peptide 1 (GLP-1) neurons of the caudal brainstem project to many brain areas, including the lateral septum (LS), which has a known role in stress responses. Previously, we showed that endogenous GLP-1 in the LS plays a physiologic role in the control of feeding under non-stressed conditions, however, central GLP-1 is also involved in behavioral and endocrine responses to stress. Here, we asked whether LS GLP-1 receptors (GLP-1R) contribute to stress-induced hypophagia. Male rats were implanted with bilateral cannulas targeting the dorsal subregion of the LS (dLS)...
March 3, 2018: Physiology & Behavior
https://www.readbyqxmd.com/read/29503858/radiosynthesis-and-evaluation-of-an-18-f-labeled-silicon-containing-exendin-4-peptide-as-a-pet-probe-for-imaging-insulinoma
#16
Lukas O Dialer, Andreas Jodal, Roger Schibli, Simon M Ametamey, Martin Béhé
Background: Analogues of exendin-4 have been radiolabeled for imaging the glucagon-like peptide type 1 receptors (GLP-1R) which are overexpressed in insulinoma. The aim of this research was to synthesize an18 F-labeled silicon containing exendin-4 peptide (18 F- 2 ) and to evaluate its in vitro and in vivo behavior in CHL-GLP-1 receptor positive tumor-bearing mice.18 F-labeled silicon containing exendin-4 peptide (18 F- 2 ) was prepared via one-step nucleophilic substitution of a silane precursor with18 F-fluoride in the presence of acetic acid and K222...
2018: EJNMMI Radiopharmacy and Chemistry
https://www.readbyqxmd.com/read/29491394/chimeric-peptide-ep45-as-a-dual-agonist-at-glp-1-and-npy2r-receptors
#17
Oleg G Chepurny, Ron L Bonaccorso, Colin A Leech, Torsten Wöllert, George M Langford, Frank Schwede, Christian L Roth, Robert P Doyle, George G Holz
We report the design and target validation of chimeric peptide EP45, a novel 45 amino acid monomeric dual agonist peptide that contains amino acid sequence motifs present within the blood glucose-lowering agent exendin-4 (Ex-4) and the appetite-suppressing agent PYY(3-36). In a new high-throughput FRET assay that provides real-time kinetic information concerning levels of cAMP in living cells, EP45 recapitulates the action of Ex-4 to stimulate cAMP production via the glucagon-like peptide-1 receptor (GLP-1R), while also recapitulating the action of PYY(3-36) to inhibit cAMP production via the neuropeptide Y2 receptor (NPY2R)...
February 28, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29487355/pancreatic-alpha-cells-in-diabetic-rats-express-active-glp-1-receptor-endosomal-co-localization-of-glp-1-glp-1r-complex-functioning-through-intra-islet-paracrine-mechanism
#18
Koji Nakashima, Hideaki Kaneto, Masashi Shimoda, Tomohiko Kimura, Kohei Kaku
Glucagon-like peptide-1 (GLP-1) stimulates insulin secretion from pancreatic beta cells and suppresses glucagon secretion from alpha cells. It remains controversial, however, whether GLP-1 receptor (GLP-1R) is expressed in mature alpha cells. In this study, unlike previous studies using non-diabetic animals, we demonstrated using diabetic model rats and confocal laser scanning microscopy that the GLP-1/GLP-1R complex was located in the endosome of diabetic islets. In addition, we showed that GLP-1 and GLP-1R co-localized with various endosomal markers and adenylate cyclase in the alpha cells of diabetic rats...
February 27, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29484377/glp%C3%A2-1r-agonists-ameliorate-peripheral-nerve-dysfunction-and-inflammation-via-p38-mapk-nf%C3%A2-%C3%AE%C2%BAb-signaling-pathways-in-streptozotocin%C3%A2-induced-diabetic-rats
#19
Jingjing Ma, Min Shi, Xiangcheng Zhang, Xiaoning Liu, Juan Chen, Ridong Zhang, Xingzhou Wang, Hong Zhang
The present study aimed to investigate the mechanism of glucagon‑like peptide‑1 receptor (GLP‑1R) agonists in the progression of diabetic peripheral neuropathy (DPN) in streptozotocin (STZ)‑induced diabetic rats, through inflammatory signaling pathways. The DPN rat model was generated by intraperitoneal injection of STZ and then treated with the GLP‑1R agonist liraglutide or saline for 8 weeks. These animals were randomly divided into 4 groups (10 rats in each): The normal control + saline group, the normal control + liraglutide group, the diabetic + saline (DM) group and the diabetic + liraglutide (DML) group...
February 23, 2018: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29481915/cognitive-dysfunction-and-metabolic-comorbidities-in-mood-disorders-a-repurposing-opportunity-for-glucagon-like-peptide-1-receptor-agonists
#20
REVIEW
Rodrigo B Mansur, Yena Lee, Mehala Subramaniapillai, Elisa Brietzke, Roger S McIntyre
Major depressive disorder and bipolar disorder are highly prevalent and disabling conditions. Cognition is considered a core domain of their psychopathology and a principle mediator of psychosocial impairment, disproportionately accounting for overall illness-associated costs. There are few interventions with replicated evidence of efficacy in treating cognitive deficits in mood disorders. Evidence also indicates that cognitive deficits are associated with obesity and involve significant impairment across multiple domains...
February 23, 2018: Neuropharmacology
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