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Exendin-4

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https://www.readbyqxmd.com/read/29045658/exendin-4-a-glucagon-like-peptide-1-receptor-agonist-attenuates-breast-cancer-growth-by-inhibiting-nf-%C3%AE%C2%BAb-activation
#1
Chikayo Iwaya, Takashi Nomiyama, Shiho Komatsu, Takako Kawanami, Yoko Tsutsumi, Yuriko Hamaguchi, Tsuyoshi Horikawa, Yasuteru Yoshinaga, Shinichi Yamashita, Tomoko Tanaka, Yuichi Terawaki, Makito Tanabe, Kazuki Nabeshima, Akinori Iwasaki, Toshihiko Yanase
Incretin therapies have received significant attention because of their tissue-protective effects, which extend beyond those associated with glycemic control. Cancer is a primary cause of death in patients with diabetes mellitus. We previously reported anti-prostate cancer effects of the glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) agonist exendin-4 (Ex-4). Breast cancer is one of the most common cancers in female patients with type 2 diabetes mellitus and obesity. Thus, we examined whether GLP-1 action could attenuate breast cancer...
October 13, 2017: Endocrinology
https://www.readbyqxmd.com/read/29042458/exenatide-modulates-tumor-endothelial-cell-interactions-in-human-ovarian-cancer-cells
#2
Agnieszka Kosowska, Enrique Gallego-Colon, Wojciech Garczorz, Agnieszka Klych-Ratuszny, Mohammad Reza F Aghdam, Michal Wozniak, Andrzej Witek, Agnieszka Wroblewska-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 of ovarian cancer which have associated worse prognosis, reduced survival and shorter relapse-free survival. Incretin drugs such as Exenatide, a synthetic analogue of Exendin-4, and Liraglutide are used as therapy for the type 2 diabetes (T2D). We studied the effects of GLP-1 and Exendin-4 on migration, apoptosis and metalloproteinase production in two human ovarian cancer cells (SKOV-3 and CAOV-3)...
October 17, 2017: Endocrine Connections
https://www.readbyqxmd.com/read/29040320/circulating-microrna-375-as-biomarker-of-pancreatic-beta-cell-death-and-protection-of-beta-cell-mass-by-cytoprotective-compounds
#3
Imane Song, Sarah Roels, Geert A Martens, Luc Bouwens
OBJECTIVE: Previous studies demonstrated that circulating microRNA-375 (miR-375) is a suitable plasma biomarker for real-time detection of beta cell death. The present study evaluated the use of this biomarker to assess the beta cytoprotective effect of phenylpropenoic acid glucoside (PPAG), which was previously demonstrated to protect beta cells against various types of injury, and of exendin-4, which is an established antidiabetic drug. METHODS: PPAG or exendin-4 were administered in mice treated with streptozotocin (STZ) to acutely induce beta cell death...
2017: PloS One
https://www.readbyqxmd.com/read/29022064/proinflammatory-switch-from-g%C3%AE-s-to-g%C3%AE-i-signaling-by-glucagon-like-peptide-1-receptor-in-murine-splenic-monocyte-following-burn-injury
#4
Qing-Hong Zhang, Ji-Wei Hao, Guang-Lei Li, Xiao-Jing Ji, Xu-Dong Yao, Ning Dong, Yong-Ming Yao
OBJECTIVE: Glucagon-like peptide-1 (GLP-1)-based therapy via G protein-coupled receptor (GPCR) GLP-1R, to attenuate hyperglycemia in critical care has attracted great attention. However, the exaggerated inflammation by GLP-1R agonist, Exendin-4, in a mouse model of burn injury was quite unexpected. Recent studies found that GPCR might elicit proinflammatory effects by switching from Gαs to Gαi signaling in the immune system. Thus, we aimed to investigate the possible Gαs to Gαi switch in GLP-1R signaling in monocyte following burn injury...
October 11, 2017: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/28986282/exendin-4-attenuates-neuronal-death-via-glp-1r-pi3k-akt-pathway-in-early-brain-injury-after-subarachnoid-hemorrhage-in-rats
#5
Zhiyi Xie, Budbazar Enkhjargal, Lingyun Wu, Keren Zhou, Chengmei Sun, Xin Hu, Vadim Gospodarev, Jiping Tang, Chao You, John H Zhang
Neuronal apoptosis is considered to be a crucial therapeutic target against early brain injury (EBI) after subarachnoid hemorrhage (SAH). Emerging evidence indicates that Exendin-4 (Ex-4), a glucagon-like peptide 1 receptor (GLP-1R) agonist, plays a neuroprotective role in cerebrovascular disease. This study was conducted in order to verify the neuroprotective role of EX-4 in EBI after SAH in rats. The endovascular perforation model of SAH was performed in Sprague-Dawley rats (n = 153). Ex-4 was intraperitoneally injected 1 h after SAH induction in the rats (SAH + Ex-4)...
October 4, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28953210/99mtc-exendin-9-39-octreotide-biokinetics-and-radiation-dosimetry-in-healthy-individuals
#6
Blanca E Ocampo-García, Clara L Santos-Cuevas, Myrna A Luna-Gutiérrez, Eleazar Ignacio-Alvarez, Martha Pedraza-López, Cesar Manzano-Mayoral
AIM: About 90% of insulinomas are benign and 5-15% are malignant. Benign insulinomas express the glucagon-like peptide-1 receptor (GLP-1R, which recognizes exendin-4 and low levels of the somatostatin receptor (SSTR, which recognizes octreotide), whereas malignant insulinomas overexpress SSTR and low levels of GLP-1R. Recently, Lys(Tc-EDDA/HYNIC)-exendin(9-39)/Tc-EDDA/HYNIC-Tyr-octreotide was formulated to detect 100% of insulinomas. The aim of this study was to estimate the biokinetics and dosimetry of Tc-exendin(9-39)/octreotide in four healthy individuals...
November 2017: Nuclear Medicine Communications
https://www.readbyqxmd.com/read/28947919/glucagon-like-peptide-1-receptor-agonist-exendin-4-protects-against-interleukin-1%C3%AE-mediated-inhibition-of-glucose-stimulated-insulin-secretion-by-mouse-insulinoma-%C3%AE-cells
#7
Ben Niu, Chao Li, Heng Su, Qingzhu Li, Qiu He, Lijuan Liu, Yuanming Xue, Tao Shen, Xueshan Xia
The aim of the present study was to investigate the protective effect of the glucagon-like peptide-1 receptor agonist exendin-4 on the interleukin (IL)-1β-induced impairment of glucose-stimulated insulin secretion (GSIS) in β-TC-6 cells. β-TC-6 cells were pretreated with various concentrations of IL-1β (0.15, 1.5 or 15 ng/ml) and exendin-4 (0.1 or 1 mM). Exendin-4 was administered to β-TC-6 cells prior to, during and following pretreatment. Cells were stimulated with various concentrations of glucose (0, 1...
September 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28947828/fenugreek-compound-n55-lowers-plasma-glucose-through-the-enhancement-of-response-of-physiological-glucagon-like-peptide-1
#8
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/28945431/micellar-nanomedicine-of-novel-fatty-acid-modified-xenopus-glucagon-like-peptide-1-improved-physicochemical-characteristics-and-therapeutic-utilities-for-type-2-diabetes
#9
Jing Han, Yingying Fei, Feng Zhou, Xinyu Chen, Weiwei Zheng, Junjie Fu
To develop novel long-acting antidiabetics with improved therapeutic efficacy, two glucagon-like peptide-1 (GLP-1) analogs were constructed through the hybridization of key sequences of GLP-1, xenGLP-1B, exendin-4 and lixisenatide. Hybrids 1 and 2 demonstrated enhanced in vitro and in vivo biological activities, and were further site-specifically lipidized at lysine residues to achieve prolonged duration of action and less frequent administration. Compared with their native peptides, compounds 3-6 showed similar in vitro activities but impaired in vivo acute hypoglycemic potencies due to decreased aqueous solubility and retarded absorption in vivo...
September 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28938428/glp-1-receptor-activation-inhibits-palmitate-induced-apoptosis-via-ceramide-in-human-cardiac-progenitor-cells
#10
Anna Leonardini, Rossella D'Oria, Maria Angela Incalza, Cristina Caccioppoli, Valentina Andrulli Buccheri, Angelo Cignarelli, Domenico Paparella, Vito Margari, Annalisa Natalicchio, Sebastio Perrini, Francesco Giorgino, Luigi Laviola
Context: Increased apoptosis of cardiomyocytes and cardiac progenitor cells (CPCs) in response to saturated fatty acids (SFA) can lead to myocardial damage and dysfunction. Ceramides mediate lipotoxicity-induced apoptosis. GLP-1 receptor (GLP1R) agonists exert beneficial effects on cardiac cells in experimental models. Objective: To investigate the protective effects of GLP1R activation on SFA-mediated apoptotic death of human CPCs. Design: Human CPCs were isolated from cardiac appendages of non-diabetic donors and then exposed to palmitate with or without pre-treatment with the GLP1R agonist exendin-4...
August 16, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28932183/plant-polyphenols-and-exendin-4-prevent-hyperactivity-and-tnf-%C3%AE-release-in-lps-treated-in-vitro-neuron-astrocyte-microglial-networks
#11
Francesca Gullo, Michela Ceriani, Alessia D'Aloia, Enzo Wanke, Andrew Constanti, Barbara Costa, Marzia Lecchi
Increasing evidence supports a decisive role for neuroinflammation in the neurodegenerative process of several central nervous system (CNS) disorders. Microglia are essential mediators of neuroinflammation and can regulate a broad spectrum of cellular responses by releasing reactive oxygen intermediates, nitric oxide, proteases, excitatory amino acids, and cytokines. We have recently shown that also in ex-vivo cortical networks of neurons, astrocytes and microglia, an increased level of tumor necrosis factor-alpha (TNF-α) was detected a few hours after exposure to the bacterial endotoxin lipopolysaccharide (LPS)...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28928089/in-vitro-and-in-vivo-studies-supporting-the-therapeutic-potential-of-zp3022-in-diabetes
#12
Jolanta Skarbaliene, Kristoffer T Rigbolt, Keld Fosgerau, Nils Billestrup
GLP-1-gastrin dual agonist ZP3022 has been shown to increase β-cell mass with a concomitant improvement of glycemic control in diabetic mice and rats. Here we tested the in-vitro effects of ZP3022 on β-cell proliferation, islet apoptosis and glucose-stimulated insulin secretion (GSIS) in rat islets of Langerhans. Moreover, gene expression profiling in whole pancreas from Zucker Diabetic Fatty (ZDF) rats was performed to characterize genes differently regulated by short-term treatment with ZP3022. Treatments with exendin-4, gastrin-17 alone or in combination were included in the studies...
September 18, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28927992/protective-effects-of-the-glp-1-mimetic-exendin-4-in-parkinson-s-disease
#13
REVIEW
Dilan Athauda, Thomas Foltynie
There is increasing interest in the potential role of glucagon-like peptide-1 (GLP-1) receptor agonists as neuroprotective treatments in neurodegenerative diseases including Parkinson's disease following the publication of the results of the Exenatide-PD trial. Of the current GLP-1 receptor agonists already licensed to treat Type 2 diabetes several including exenatide, liraglutide and lixisenatide are the subject of ongoing clinical trials in PD. The underlying rationale for using drugs licensed and effective for T2DM in PD patients therefore needs to be scrutinized, and the results obtained to date critically reviewed...
September 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28927802/synthesis-and-biological-evaluation-of-an-111-in-labeled-exendin-4-derivative-as-a-single-photon-emission-computed-tomography-probe-for-imaging-pancreatic-%C3%AE-cells
#14
Hiroyuki Kimura, Naotaka Fujita, Kaori Kanbe, Hirokazu Matsuda, Hiroyuki Watanabe, Kenji Arimitsu, Hiroyuki Fujimoto, Keita Hamamatsu, Yusuke Yagi, Masahiro Ono, Nobuya Inagaki, Hideo Saji
A non-invasive method of pancreatic β-cell mass measurement is needed to enhance our understanding of the pathogenesis of diabetes, facilitate the early diagnosis of this disease, and promote the development of novel therapeutics. Here, we described the synthesis of a novel indium-111 ((111)In) exendin-4 derivative, [Lys(12)(In-BnDTPA-Ahx)]exendin-4, through a process involving isothiocyanate-benzyl-DTPA (BnDTPA) and 6-aminohexanoic acid (Ahx) attached to an ɛ-amino group at the lysine-12 residue. We further evaluated the potential use of this derivative as a SPECT probe for pancreatic β-cell imaging...
September 7, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28920919/age-dependent-human-%C3%AE-cell-proliferation-induced-by-glucagon-like-peptide-1-and-calcineurin-signaling
#15
Chunhua Dai, Yan Hang, Alena Shostak, Greg Poffenberger, Nathaniel Hart, Nripesh Prasad, Neil Phillips, Shawn E Levy, Dale L Greiner, Leonard D Shultz, Rita Bottino, Seung K Kim, Alvin C Powers
Inadequate pancreatic β cell function underlies type 1 and type 2 diabetes mellitus. Strategies to expand functional cells have focused on discovering and controlling mechanisms that limit the proliferation of human β cells. Here, we developed an engraftment strategy to examine age-associated human islet cell replication competence and reveal mechanisms underlying age-dependent decline of β cell proliferation in human islets. We found that exendin-4 (Ex-4), an agonist of the glucagon-like peptide 1 receptor (GLP-1R), stimulates human β cell proliferation in juvenile but not adult islets...
October 2, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28912645/anti-inflammatory-effect-of-glucagon-like-peptide-1-receptor-agonist-exendin-4-through-modulation-of-ib1-jip1-expression-and-jnk-signaling-in-stroke
#16
Soojin Kim, Jaewon Jeong, Hye-Seon Jung, Bokyung Kim, Ye-Eun Kim, Da-Sol Lim, So-Dam Kim, Yun Seon Song
Glucagon like peptide-1 (GLP-1) stimulates glucose-dependent insulin secretion. Dipeptidyl peptidase-4 (DPP-4) inhibitors, which block inactivation of GLP-1, are currently in clinical use for type 2 diabetes mellitus. Recently, GLP-1 has also been reported to have neuroprotective effects in cases of cerebral ischemia. We therefore investigated the neuroprotective effects of GLP-1 receptor (GLP-1R) agonist, exendin-4 (ex-4), after cerebral ischemia-reperfusion injury. Transient middle cerebral artery occlusion (tMCAO) was induced in rats by intracerebroventricular (i...
August 2017: Experimental Neurobiology
https://www.readbyqxmd.com/read/28900935/metabolic-disorders-and-cancer-hepatocyte-store-operated-ca-2-channels-in-nonalcoholic-fatty-liver-disease
#17
Eunüs S Ali, Grigori Y Rychkov, Greg J Barritt
In steatotic hepatocytes, intracellular Ca(2+) homeostasis is substantially altered compared to normal. Decreased Ca(2+) in the endoplasmic reticulum (ER) can lead to ER stress, an important mediator of the progression of liver steatosis to nonalcoholic steatohepatitis, type 2 diabetes, and hepatocellular carcinoma. Store-operated Ca(2+) channels (SOCs) in hepatocytes are composed principally of Orai1 and STIM1 proteins. Their main role is the maintenance of adequate Ca(2+) in the lumen of the ER. In steatotic hepatocytes, store-operated Ca(2+) entry (SOCE) is substantially inhibited...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28891030/species-differences-in-pancreatic-binding-of-do3a-vs-cys-40-exendin4
#18
Olof Eriksson, Ulrika Rosenström, Ram K Selvaraju, Barbro Eriksson, Irina Velikyan
AIMS: Radiolabeled Exendin-4 has been proposed as suitable imaging marker for pancreatic beta cell mass quantification mediated by Glucagon-like peptide-1 receptor (GLP-1R). However, noticeable species variations in basal pancreatic uptake as well as uptake reduction degree due to selective beta cell ablation were observed. METHODS: In vitro and ex vivo autoradiography studies of pancreas were performed using [(177)Lu]Lu-DO3A-VS-Cys(40)-Exendin4, in order to investigate the mechanism of uptake as well as the islet uptake contrast in mouse, rat, pig, and non-human primate...
November 2017: Acta Diabetologica
https://www.readbyqxmd.com/read/28846695/novel-and-ultra-rare-damaging-variants-in-neuropeptide-signaling-are-associated-with-disordered-eating-behaviors
#19
Michael Lutter, Ethan Bahl, Claire Hannah, Dabney Hofammann, Summer Acevedo, Huxing Cui, Carrie J McAdams, Jacob J Michaelson
OBJECTIVE: Eating disorders develop through a combination of genetic vulnerability and environmental stress, however the genetic basis of this risk is unknown. METHODS: To understand the genetic basis of this risk, we performed whole exome sequencing on 93 unrelated individuals with eating disorders (38 restricted-eating and 55 binge-eating) to identify novel damaging variants. Candidate genes with an excessive burden of predicted damaging variants were then prioritized based upon an unbiased, data-driven bioinformatic analysis...
2017: PloS One
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
#20
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...
August 23, 2017: Amino Acids
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