Metabolic responses and benefits of glucagon‐like peptide‐1 (GLP‐1) receptor ligands

Once-Weekly Semaglutide in Adults with Overweight or Obesity

(2021) John P.H. Wilding et al.   NEW ENGLAND JOURNAL OF MEDICINE

L-Cell Differentiation Is Induced by Bile Acids Through GPBAR1 and Paracrine GLP-1 and Serotonin Signaling

(2020) Mari Lilith Lund et al.   DIABETES

Emerging role of GIP and related gut hormones in fertility and PCOS

(2020) R. Charlotte Moffett et al.   PEPTIDES

Selective stimulation of colonic L cells improves metabolic outcomes in mice

(2020) Jo E. Lewis et al.   DIABETOLOGIA

Enteroendocrine K‐cells exert complementary effects to control bone quality and mass in mice

(2020) B. Gobron et al.   JOURNAL OF BONE AND MINERAL RESEARCH

Liraglutide and sitagliptin counter beta- to alpha-cell transdifferentiation in diabetes

(2020) Neil Tanday et al.   JOURNAL OF ENDOCRINOLOGY

Liraglutide treatment improves endothelial function in the Ldlr−/− mouse model of atherosclerosis and affects genes involved in vascular remodelling and inflammation

(2020) Katrine Dahl Bjørnholm et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

The renal extraction and the natriuretic action of GLP-1 in humans depend on interaction with the GLP-1 receptor

(2020) Ali Asmar et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Chronic glucose-dependent insulinotropic polypeptide receptor (GIPR) agonism desensitizes adipocyte GIPR activity mimicking functional GIPR antagonism

(2020) Elizabeth A. Killion et al.   Nature Communications

GLP-1 receptor agonist ameliorates experimental lung fibrosis

(2020) Juan Fandiño et al.   Scientific Reports

A Placebo-Controlled Trial of Subcutaneous Semaglutide in Nonalcoholic Steatohepatitis

(2020) Philip N. Newsome et al.   NEW ENGLAND JOURNAL OF MEDICINE

The GLP-1 Receptor Agonist Exenatide Ameliorates Bone Composition and Tissue Material Properties in High Fat Fed Diabetic Mice

(2019) Sity Aishah Mansur et al.   Frontiers in Endocrinology

Advances in the physiology of gastric emptying

(2019) Raj K. Goyal et al.   NEUROGASTROENTEROLOGY AND MOTILITY

Extracellular fluid volume expansion uncovers a natriuretic action of GLP-1: a functional GLP-1-renal axis in man

(2019) Ali Asmar et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

The efficacy and safety of exenatide once weekly in patients with type 2 diabetes

(2019) Sebastian M. Heimbürger et al.   EXPERT OPINION ON PHARMACOTHERAPY

Glucagon‐like peptide‐1 receptor agonists and risk of bone fracture in patients with type 2 diabetes: A meta‐analysis of randomized controlled trials

(2019) Liang Cheng et al.   DIABETES-METABOLISM RESEARCH AND REVIEWS

PIONEER 1: Randomized Clinical Trial of the Efficacy and Safety of Oral Semaglutide Monotherapy in Comparison With Placebo in Patients With Type 2 Diabetes

(2019) Vanita R. Aroda et al.   DIABETES CARE

Oral semaglutide versus subcutaneous liraglutide and placebo in type 2 diabetes (PIONEER 4): a randomised, double-blind, phase 3a trial

(2019) Richard Pratley et al.   LANCET

Efficacy and safety of once-weekly semaglutide 1.0 mg vs once-daily liraglutide 1.2 mg as add-on to 1–3 oral antidiabetic drugs in subjects with type 2 diabetes (SUSTAIN 10)

(2019) M.S. Capehorn et al.   DIABETES & METABOLISM

Mechanistic insights regarding the role of SGLT2 inhibitors and GLP1 agonist drugs on cardiovascular disease in diabetes

(2019) Vinay Garg et al.   PROGRESS IN CARDIOVASCULAR DISEASES

The GLP1R Agonist Liraglutide Reduces Hyperglucagonemia Induced by the SGLT2 Inhibitor Dapagliflozin via Somatostatin Release

(2019) Chiara Saponaro et al.   Cell Reports

Neuroprotection in Rats Following Ischaemia-Reperfusion Injury by GLP-1 Analogues—Liraglutide and Semaglutide

(2019) Maryna V. Basalay et al.   CARDIOVASCULAR DRUGS AND THERAPY

GIP and the gut-bone axis – Physiological, pathophysiological and potential therapeutic implications

(2019) Signe Stensen et al.   PEPTIDES

Blockade of gastric inhibitory polypeptide (GIP) action as a novel means of countering insulin resistance in the treatment of obesity-diabetes

(2019) Nigel Irwin et al.   PEPTIDES

GIP analogues augment bone strength by modulating bone composition in diet-induced obesity in mice

(2019) Sagar S. Vyavahare et al.   PEPTIDES

The core clock gene, Bmal1, and its downstream target, the SNARE regulatory protein secretagogin, are necessary for circadian secretion of glucagon-like peptide-1

(2019) Andrew D. Biancolin et al.   Molecular Metabolism

Novel dual incretin agonist peptide with antidiabetic and neuroprotective potential

(2018) N.M. Pathak et al.   BIOCHEMICAL PHARMACOLOGY

Clinical application of glucagon-like peptide-1 receptor agonists in cardiovascular disease: lessons from recent clinical cardiovascular outcomes trials

(2018) Atsushi Tanaka et al.   Cardiovascular Diabetology

A review of GLP-1 receptor agonists: Evolution and advancement, through the lens of randomised controlled trials

(2018) Vanita R. Aroda   DIABETES OBESITY & METABOLISM

Semaglutide: First Global Approval

(2018) Sohita Dhillon   DRUGS

A novel GLP-1/xenin hybrid peptide improves glucose homeostasis, circulating lipids and restores GIP sensitivity in high fat fed mice

(2018) Annie Hasib et al.   PEPTIDES

Cardiovascular outcomes with glucagon-like peptide-1 receptor agonists in patients with type 2 diabetes: a meta-analysis

(2018) M Angelyn Bethel et al.   Lancet Diabetes & Endocrinology

An incretin-based tri-agonist promotes superior insulin secretion from murine pancreatic islets via PLC activation

(2018) Noushafarin Khajavi et al.   CELLULAR SIGNALLING

Efficacy of targeting bone-specific GIP receptor in ovariectomy-induced bone loss

(2018) Guillaume Mabilleau et al.   JOURNAL OF ENDOCRINOLOGY

Sitagliptin Alters Bone Composition in High-Fat-Fed Mice

(2018) Sity Aishah Mansur et al.   CALCIFIED TISSUE INTERNATIONAL

Oral semaglutide for the treatment of type 2 diabetes

(2018) Maka S. Hedrington et al.   EXPERT OPINION ON PHARMACOTHERAPY

Twice the benefits with twincretins?

(2018) Michael Stumvoll et al.   LANCET

Anti-obesity effects of GIPR antagonists alone and in combination with GLP-1R agonists in preclinical models

(2018) Elizabeth A. Killion et al.   Science Translational Medicine

Transcellular stomach absorption of a derivatized glucagon-like peptide-1 receptor agonist

(2018) Stephen T. Buckley et al.   Science Translational Medicine

LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept

(2018) Tamer Coskun et al.   Molecular Metabolism

Regulation of Endogenous (Male) Rodent GLP-1 Secretion and Human Islet Insulin Secretion by Antagonism of Somatostatin Receptor 5

(2017) Thomas B Farb et al.   ENDOCRINOLOGY

Age-dependent human β cell proliferation induced by glucagon-like peptide 1 and calcineurin signaling

(2017) Chunhua Dai et al.   JOURNAL OF CLINICAL INVESTIGATION

Novel skeletal effects of glucagon-like peptide-1 (GLP-1) receptor agonists

(2017) Guillaume Mabilleau et al.   JOURNAL OF ENDOCRINOLOGY

Effects of Once-Weekly Exenatide on Cardiovascular Outcomes in Type 2 Diabetes

(2017) Rury R. Holman et al.   NEW ENGLAND JOURNAL OF MEDICINE

The autonomic nervous system and cardiac GLP-1 receptors control heart rate in mice

(2017) Laurie L. Baggio et al.   Molecular Metabolism

Monomeric GLP-1/GIP/glucagon triagonism corrects obesity, hepatosteatosis, and dyslipidemia in female mice

(2017) Sigrid Jall et al.   Molecular Metabolism

Glucose-dependent insulinotropic polypeptide (GIP) dose-dependently reduces osteoclast differentiation and resorption

(2016) Guillaume Mabilleau et al.   BONE

Gastrointestinal actions of glucagon-like peptide-1-based therapies: glycaemic control beyond the pancreas

(2016) M. M. Smits et al.   DIABETES OBESITY & METABOLISM

Successful Pregnancy after Improving Insulin Resistance with the Glucagon-Like Peptide-1 Analogue in a Woman with Polycystic Ovary Syndrome: A Case Report and Review of the Literature

(2016) Qianying Yang et al.   GYNECOLOGIC AND OBSTETRIC INVESTIGATION

Liraglutide safety and efficacy in patients with non-alcoholic steatohepatitis (LEAN): a multicentre, double-blind, randomised, placebo-controlled phase 2 study

(2016) Matthew James Armstrong et al.   LANCET

Semaglutide and Cardiovascular Outcomes in Patients with Type 2 Diabetes

(2016) Steven P. Marso et al.   NEW ENGLAND JOURNAL OF MEDICINE

Liraglutide and Cardiovascular Outcomes in Type 2 Diabetes

(2016) Steven P. Marso et al.   NEW ENGLAND JOURNAL OF MEDICINE

Effects of Exenatide on Metabolic Changes, Sexual Hormones, Inflammatory Cytokines, Adipokines, and Weight Change in a DHEA-Treated Rat Model

(2016) Lingjun Sun et al.   Reproductive Sciences

GLP-1 Receptor Agonist Exenatide Attenuates the Detrimental Effects of Obesity on Inflammatory Profile in Testis and Sperm Quality in Mice

(2015) Erhong Zhang et al.   AMERICAN JOURNAL OF REPRODUCTIVE IMMUNOLOGY

Effect of the glucagon-like peptide-1 analogue liraglutide on coronary microvascular function in patients with type 2 diabetes – a randomized, single-blinded, cross-over pilot study

(2015) Rebekka Faber et al.   Cardiovascular Diabetology

GLP-1R Agonists Modulate Enteric Immune Responses Through the Intestinal Intraepithelial Lymphocyte GLP-1R

(2015) Bernardo Yusta et al.   DIABETES

A Novel CCK-8/GLP-1 Hybrid Peptide Exhibiting Prominent Insulinotropic, Glucose-Lowering, and Satiety Actions With Significant Therapeutic Potential in High-Fat–Fed Mice

(2015) Nigel Irwin et al.   DIABETES

Contrasting Effects of Lixisenatide and Liraglutide on Postprandial Glycemic Control, Gastric Emptying, and Safety Parameters in Patients With Type 2 Diabetes on Optimized Insulin Glargine With or Without Metformin: A Randomized, Open-Label Trial

(2015) Juris J. Meier et al.   DIABETES CARE

Impact of GLP-1 receptor agonists on blood pressure, heart rate and hypertension among patients with type 2 diabetes: A systematic review and network meta-analysis

(2015) Feng Sun et al.   DIABETES RESEARCH AND CLINICAL PRACTICE

Stable Incretin Mimetics Counter Rapid Deterioration of Bone Quality in Type 1 Diabetes Mellitus

(2015) Sity Aishah Mansur et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Distribution and characterisation of Glucagon-like peptide-1 receptor expressing cells in the mouse brain

(2015) Simon C. Cork et al.   Molecular Metabolism

GLP-1 Receptor Localization in Monkey and Human Tissue: Novel Distribution Revealed With Extensively Validated Monoclonal Antibody

(2014) Charles Pyke et al.   ENDOCRINOLOGY

The short chain fatty acid propionate stimulates GLP-1 and PYY secretion via free fatty acid receptor 2 in rodents

(2014) A Psichas et al.   INTERNATIONAL JOURNAL OF OBESITY

Glucagon-like-peptide-1 receptor expression in normal and diseased human thyroid and pancreas

(2014) Beatrice Waser et al.   MODERN PATHOLOGY

Incretin Receptor Null Mice Reveal Key Role of GLP-1 but Not GIP in Pancreatic Beta Cell Adaptation to Pregnancy

(2014) R. Charlotte Moffett et al.   PLoS One

Inactivation of the cardiomyocyte glucagon-like peptide-1 receptor (GLP-1R) unmasks cardiomyocyte-independent GLP-1R-mediated cardioprotection

(2014) John R. Ussher et al.   Molecular Metabolism

GLP-1 increases microvascular recruitment but not glucose uptake in human and rat skeletal muscle

(2013) Kim A. Sjøberg et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Pharmacology, Physiology, and Mechanisms of Incretin Hormone Action

(2013) Jonathan E. Campbell et al.   Cell Metabolism

Glucagon-Like Peptide-1 Protects Against Cardiac Microvascular Injury in Diabetes via a cAMP/PKA/Rho-Dependent Mechanism

(2013) D. Wang et al.   DIABETES

Identification and Characterization of GLP-1 Receptor-Expressing Cells Using a New Transgenic Mouse Model

(2013) P. Richards et al.   DIABETES

Oligopeptides stimulate glucagon-like peptide-1 secretion in mice through proton-coupled uptake and the calcium-sensing receptor

(2013) Eleftheria Diakogiannaki et al.   DIABETOLOGIA

A DPP-IV-resistant triple-acting agonist of GIP, GLP-1 and glucagon receptors with potent glucose-lowering and insulinotropic actions in high-fat-fed mice

(2013) V. K. Bhat et al.   DIABETOLOGIA

Orall-Arginine Stimulates GLP-1 Secretion to Improve Glucose Tolerance in Male Mice

(2013) Christoffer Clemmensen et al.   ENDOCRINOLOGY

A Novel Glucagon-like Peptide-1 (GLP-1)/Glucagon Hybrid Peptide with Triple-acting Agonist Activity at Glucose-dependent Insulinotropic Polypeptide, GLP-1, and Glucagon Receptors and Therapeutic Potential in High Fat-fed Mice

(2013) Victor A. Gault et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Glucagon-Like Peptide-1 (GLP-1): Effect on Kidney Hemodynamics and Renin-Angiotensin-Aldosterone System in Healthy Men

(2013) Jeppe Skov et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Optimal bone mechanical and material properties require a functional glucagon-like peptide-1 receptor

(2013) Guillaume Mabilleau et al.   JOURNAL OF ENDOCRINOLOGY

The protective roles of GLP-1R signaling in diabetic nephropathy: possible mechanism and therapeutic potential

(2013) Hiroki Fujita et al.   KIDNEY INTERNATIONAL

GLP-1 receptor activation and Epac2 link atrial natriuretic peptide secretion to control of blood pressure

(2013) Minsuk Kim et al.   NATURE MEDICINE

The effect of RAAS blockade on the progression of diabetic nephropathy

(2013) Sara S. Roscioni et al.   Nature Reviews Nephrology

Unimolecular Dual Incretins Maximize Metabolic Benefits in Rodents, Monkeys, and Humans

(2013) B. Finan et al.   Science Translational Medicine

Effects of exenatide and liraglutide on heart rate, blood pressure and body weight: systematic review and meta-analysis

(2013) Louise E Robinson et al.   BMJ Open

Predominant role of active versus facilitative glucose transport for glucagon-like peptide-1 secretion

(2012) H. E. Parker et al.   DIABETOLOGIA

The Glucagon-Like Peptide-1 Receptor—or Not?

(2012) Charles Pyke et al.   ENDOCRINOLOGY

GIP Does Not Potentiate the Antidiabetic Effects of GLP-1 in Hyperglycemic Patients With Type 2 Diabetes

(2011) N. Mentis et al.   DIABETES

Rapid Tachyphylaxis of the Glucagon-Like Peptide 1-Induced Deceleration of Gastric Emptying in Humans

(2011) M. A. Nauck et al.   DIABETES

Glucagon-like peptide-1 (GLP-1) and the regulation of human invariant natural killer T cells: lessons from obesity, diabetes and psoriasis

(2011) A. E. Hogan et al.   DIABETOLOGIA

Native incretins prevent the development of atherosclerotic lesions in apolipoprotein E knockout mice

(2011) M. Nagashima et al.   DIABETOLOGIA

Glutamine Triggers and Potentiates Glucagon-Like Peptide-1 Secretion by Raising Cytosolic Ca2+and cAMP

(2011) Gwen Tolhurst et al.   ENDOCRINOLOGY

GLP-1 Analogs Reduce Hepatocyte Steatosis and Improve Survival by Enhancing the Unfolded Protein Response and Promoting Macroautophagy

(2011) Shvetank Sharma et al.   PLoS One

GLP-1 Inhibits and Adrenaline Stimulates Glucagon Release by Differential Modulation of N- and L-Type Ca2+ Channel-Dependent Exocytosis

(2010) Yang Z. De Marinis et al.   Cell Metabolism

Glucagon-like peptide-1 receptor is present on human hepatocytes and has a direct role in decreasing hepatic steatosis in vitro by modulating elements of the insulin signaling pathway

(2010) Nitika Arora Gupta et al.   HEPATOLOGY

Liraglutide

(2010) Daniel J. Drucker et al.   NATURE REVIEWS DRUG DISCOVERY

Therapeutic potential for GIP receptor agonists and antagonists

(2009) Nigel Irwin et al.   BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & METABOLISM

Effects of exendin-4 on glucose tolerance, insulin secretion, and beta-cell proliferation depend on treatment dose, treatment duration and meal contents

(2009) Masayuki Arakawa et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Metabolic effects of sustained activation of the GLP-1 receptor alone and in combination with background GIP receptor antagonism in high fat-fed mice

(2009) N. Irwin et al.   DIABETES OBESITY & METABOLISM

Evidence for beneficial effects of compromised gastric inhibitory polypeptide action in obesity-related diabetes and possible therapeutic implications

(2009) N. Irwin et al.   DIABETOLOGIA

Preserved Inhibitory Potency of GLP-1 on Glucagon Secretion in Type 2 Diabetes Mellitus

(2009) Kristine J. Hare et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

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)

(2009) John B Buse et al.   LANCET

Four weeks of near-normalisation of blood glucose improves the insulin response to glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes

(2008) P. V. Højberg et al.   DIABETOLOGIA