Discovery and development of exenatide: the first antidiabetic agent to leverage the multiple benefits of the incretin hormone, GLP-1.

scientific article published on 12 December 2012

Discovery and development of exenatide: the first antidiabetic agent to leverage the multiple benefits of the incretin hormone, GLP-1. is …
instance of (P31):
review articleQ7318358
scholarly articleQ13442814

External links are
P356DOI10.1517/17460441.2013.741580
P698PubMed publication ID23231438
P5875ResearchGate publication ID233899974

P2093author name stringDavid G Parkes
Kenneth F Mace
Michael E Trautmann
P2860cites workA role for glucagon-like peptide-1 in the central regulation of feedingQ24314317
Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptorQ24318252
Expression cloning of the pancreatic beta cell receptor for the gluco-incretin hormone glucagon-like peptide 1Q24563957
Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, reverses hepatic steatosis in ob/ob miceQ24629441
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Energy intake and appetite are suppressed by glucagon-like peptide-1 (GLP-1) in obese menQ58448899
Both Subcutaneously and Intravenously Administered Glucagon-Like Peptide I Are Rapidly Degraded From the NH2-Terminus in Type II Diabetic Patients and in Healthy SubjectsQ58449089
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Exendin-4 ameliorates motor neuron degeneration in cellular and animal models of amyotrophic lateral sclerosisQ28481242
Glucagon-like peptide-1 receptor signaling modulates beta cell apoptosisQ28570314
Exendin-4 stimulates both beta-cell replication and neogenesis, resulting in increased beta-cell mass and improved glucose tolerance in diabetic ratsQ28578709
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Acute pancreatitis in type 2 diabetes treated with exenatide or sitagliptin: a retrospective observational pharmacy claims analysisQ34237350
Association of pancreatitis with glucagon-like peptide-1 agonist use.Q34618507
Pancreatitis, pancreatic, and thyroid cancer with glucagon-like peptide-1-based therapiesQ34627077
Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6).Q34986024
Four weeks of treatment with liraglutide reduces insulin dose without loss of glycemic control in type 1 diabetic patients with and without residual beta-cell functionQ35060123
Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetesQ35618856
Importance of quantifying insulin secretion in relation to insulin sensitivity to accurately assess beta cell function in clinical studiesQ35649213
Evidence of GLP-1-mediated neuroprotection in an animal model of pyridoxine-induced peripheral sensory neuropathyQ35748345
Preserved incretin activity of glucagon-like peptide 1 [7-36 amide] but not of synthetic human gastric inhibitory polypeptide in patients with type-2 diabetes mellitusQ35824086
Target-mediated pharmacokinetic and pharmacodynamic model of exendin-4 in rats, monkeys, and humansQ35913076
Physiology of GLP-1--lessons from glucoincretin receptor knockout miceQ36012473
Effect of renal impairment on the pharmacokinetics of exenatideQ36024667
Therapeutic approaches to preserve islet mass in type 2 diabetesQ36366851
Relative risk of acute pancreatitis in initiators of exenatide twice daily compared with other anti-diabetic medication: a follow-up studyQ36420499
Fatty liver: a novel component of the metabolic syndromeQ36906553
GLP-1 receptor stimulation preserves primary cortical and dopaminergic neurons in cellular and rodent models of stroke and ParkinsonismQ37078997
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The incretin system and its role in type 2 diabetes mellitusQ37266863
Glucagon-like peptide-1 can reverse the age-related decline in glucose tolerance in ratsQ37368678
Glucagon-like peptide 1 promotes satiety and suppresses energy intake in humansQ37377728
Role of the incretin pathway in the pathogenesis of type 2 diabetes mellitusQ37642377
Glucagon-like peptide 1 receptor stimulation as a means of neuroprotectionQ37686556
A cohort study of acute pancreatitis in relation to exenatide use.Q37841739
Encapsulation of exenatide in poly-(D,L-lactide-co-glycolide) microspheres produced an investigational long-acting once-weekly formulation for type 2 diabetesQ37900626
The effects of exenatide bid on metabolic control, medication use and hospitalization in patients with type 2 diabetes mellitus in clinical practice: a systematic reviewQ37954675
Glucose-lowering and insulin-sensitizing actions of exendin-4: studies in obese diabetic (ob/ob, db/db) mice, diabetic fatty Zucker rats, and diabetic rhesus monkeys (Macaca mulatta).Q38324621
Exenatide does not evoke pancreatitis and attenuates chemically induced pancreatitis in normal and diabetic rodentsQ38340339
The long-acting GLP-1 derivative NN2211 ameliorates glycemia and increases beta-cell mass in diabetic miceQ38363214
Exenatide reduces final infarct size in patients with ST-segment-elevation myocardial infarction and short-duration of ischemiaQ38473330
Inhibition of monocyte adhesion to endothelial cells and attenuation of atherosclerotic lesion by a glucagon-like peptide-1 receptor agonist, exendin-4.Q39778606
A novel neurotrophic property of glucagon-like peptide 1: a promoter of nerve growth factor-mediated differentiation in PC12 cellsQ40748616
Glucagon-like peptide-1 and the exenatide analogue AC3174 improve cardiac function, cardiac remodeling, and survival in rats with chronic heart failureQ41267217
Cardioprotective and vasodilatory actions of glucagon-like peptide 1 receptor are mediated through both glucagon-like peptide 1 receptor-dependent and -independent pathwaysQ42165735
Regulation of glucose transporters and hexose uptake in 3T3-L1 adipocytes: glucagon-like peptide-1 and insulin interactionsQ42450579
Identification of glucagon-like peptide 1 (GLP-1) actions essential for glucose homeostasis in mice with disruption of GLP-1 receptor signalingQ42454515
Altered cAMP and Ca2+ signaling in mouse pancreatic islets with glucagon-like peptide-1 receptor null phenotypeQ42478360
Glucagon-like peptide-1(7-36) amide (GLP-1) enhances insulin-stimulated glucose metabolism in 3T3-L1 adipocytes: one of several potential extrapancreatic sites of GLP-1 action.Q42492827
Glucagon-like peptide-1 and exendin-4 stimulate beta-cell neogenesis in streptozotocin-treated newborn rats resulting in persistently improved glucose homeostasis at adult age.Q42506332
Persistent improvement of type 2 diabetes in the Goto-Kakizaki rat model by expansion of the beta-cell mass during the prediabetic period with glucagon-like peptide-1 or exendin-4.Q42520650
Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4.Q42524942
The exenatide analogue AC3174 attenuates hypertension, insulin resistance, and renal dysfunction in Dahl salt-sensitive ratsQ42533774
Exenatide is non-inferior to insulin in reducing HbA1c: an integrated analysis of 1423 patients with type 2 diabetesQ42660412
Glucagon-like peptide-1 receptor activation modulates pancreatitis-associated gene expression but does not modify the susceptibility to experimental pancreatitis in miceQ43064614
The glucagon-like peptide 1 receptor is essential for postprandial lipoprotein synthesis and secretion in hamsters and miceQ43231241
Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreasQ43276184
Exenatide reduces infarct size and improves cardiac function in a porcine model of ischemia and reperfusion injuryQ43574002
Insulinotropic actions of exendin-4 and glucagon-like peptide-1 in vivo and in vitroQ43586628
Glucose competence of the hepatoportal vein sensor requires the presence of an activated glucagon-like peptide-1 receptorQ43687822
The insulinotropic effect of acute exendin-4 administered to humans: comparison of nondiabetic state to type 2 diabetesQ43913927
Glucagon-like peptide-1 treatment delays the onset of diabetes in 8 week-old db/db miceQ44145661
Glucagon-like peptide-1 promotes islet cell growth and inhibits apoptosis in Zucker diabetic rats.Q44193794
Role of endogenous glucagon-like peptide-1 in islet regeneration after partial pancreatectomyQ44286369
Neonatal exendin-4 prevents the development of diabetes in the intrauterine growth retarded rat.Q44328972
Effects of exenatide on systolic blood pressure in subjects with type 2 diabetesQ44620317
Ex vivo human placental transfer of the peptides pramlintide and exenatide (synthetic exendin-4).Q44781512
Exendin-4 normalized postcibal glycemic excursions in type 1 diabetesQ44968815
Exenatide (exendin-4) improves insulin sensitivity and {beta}-cell mass in insulin-resistant obese fa/fa Zucker rats independent of glycemia and body weightQ45200771
Exenatide improves hypertension in a rat model of the metabolic syndromeQ46042040
Exendin-4 has an anti-hypertensive effect in salt-sensitive mice modelQ46159268
Dose-response for glycaemic and metabolic changes 28 days after single injection of long-acting release exenatide in diabetic fatty Zucker ratsQ46509023
Pharmacokinetics and pharmacodynamics of exenatide following alternate routes of administrationQ46740431
Antiobesity action of peripheral exenatide (exendin-4) in rodents: effects on food intake, body weight, metabolic status and side-effect measuresQ46988910
Insulinotropic glucagon-like peptide 1 agonists stimulate expression of homeodomain protein IDX-1 and increase islet size in mouse pancreasQ47234077
Peripheral versus central effects of glucagon-like peptide-1 receptor agonists on satiety and body weight loss in Zucker obese ratsQ47235596
Enhanced glucose-dependent insulinotropic polypeptide secretion and insulinotropic action in glucagon-like peptide 1 receptor -/- miceQ47904088
The glucagon-like peptide 1 (GLP-1) analogue, exendin-4, decreases the rewarding value of food: a new role for mesolimbic GLP-1 receptors.Q47996706
Exendin-4, but not glucagon-like peptide-1, is cleared exclusively by glomerular filtration in anaesthetised pigsQ48725317
Mouse pancreatic beta-cells exhibit preserved glucose competence after disruption of the glucagon-like peptide-1 receptor geneQ50892144
The effects of 13 wk of liraglutide treatment on endocrine and exocrine pancreas in male and female ZDF rats: a quantitative and qualitative analysis revealing no evidence of drug-induced pancreatitis.Q51339510
Effects of intravenous exenatide in type 2 diabetic patients with congestive heart failure: a double-blind, randomised controlled clinical trial of efficacy and safety.Q51368060
Liraglutide as additional treatment for type 1 diabetes.Q51372390
Effects of subcutaneous glucagon-like peptide 1 (GLP-1 [7-36 amide]) in patients with NIDDM.Q51578359
Glucagonostatic actions and reduction of fasting hyperglycemia by exogenous glucagon-like peptide I(7-36) amide in type I diabetic patients.Q51581246
Truncated GLP-1 (proglucagon 78-107-amide) inhibits gastric and pancreatic functions in man.Q51601217
Glucose intolerance but normal satiety in mice with a null mutation in the glucagon-like peptide 1 receptor gene.Q52522147
Exenatide alters myocardial glucose transport and uptake depending on insulin resistance and increases myocardial blood flow in patients with type 2 diabetes.Q53163778
Investigation of exenatide elimination and its in vivo and in vitro degradation.Q53621094
P433issue2
P407language of work or nameEnglishQ1860
P304page(s)219-244
P577publication date2012-12-12
P1433published inExpert Opinion on Drug DiscoveryQ5421204
P1476titleDiscovery and development of exenatide: the first antidiabetic agent to leverage the multiple benefits of the incretin hormone, GLP-1.
P478volume8

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