Discovery of a potent GIPR peptide antagonist that is effective in rodent and human systems

The GIPR is Predominantly Localized to Non-Adipocyte Cell Types Within White Adipose Tissue

(2022) Jonathan E. Campbell et al.   DIABETES

Acute concomitant GIP receptor antagonism during GLP ‐1 receptor agonism does not affect appetite, resting energy expenditure or food intake in patients with type 2 diabetes and overweight/obesity

(2022) Signe Stensen et al.   DIABETES OBESITY & METABOLISM

Glucose‐dependent insulinotropic polypeptide receptor antagonist treatment causes a reduction in weight gain in ovariectomised high fat diet‐fed mice

(2022) Geke Aline Boer et al.   BRITISH JOURNAL OF PHARMACOLOGY

Next generation GLP-1/GIP/glucagon triple agonists normalize body weight in obese mice

(2022) Patrick J. Knerr et al.   Molecular Metabolism

The glucose-dependent insulinotropic polypeptide (GIP) regulates body weight and food intake via CNS-GIPR signaling

(2021) Qian Zhang et al.   Cell Metabolism

Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists

(2021) Bin Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chronic peptide-based GIP receptor inhibition exhibits modest glucose metabolic changes in mice when administered either alone or combined with GLP-1 agonism

(2021) Jason A. West et al.   PLoS One

Investigating GIPR (ant)agonism: A structural analysis of GIP and its receptor

(2021) Florent X. Smit et al.   STRUCTURE

Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes

(2021) Juan P. Frías et al.   NEW ENGLAND JOURNAL OF MEDICINE

Efficacy and tolerability of tirzepatide, a dual glucose‐dependent insulinotropic peptide and glucagon‐like peptide‐1 receptor agonist in patients with type 2 diabetes: A 12‐week, randomized, double‐blind, placebo‐controlled study to evaluate different dose‐escalation regimens

(2020) Juan Pablo Frias et al.   DIABETES OBESITY & 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

GIP(3-30)NH2 – a tool for the study of GIP physiology

(2020) Mads Bank Lynggaard et al.   CURRENT OPINION IN PHARMACOLOGY

The Role of Tirzepatide, Dual GIP and GLP-1 Receptor Agonist, in the Management of Type 2 Diabetes: The SURPASS Clinical Trials

(2020) Thinzar Min et al.   Diabetes Therapy

Temporal plasticity of insulin and incretin secretion and insulin sensitivity following sleeve gastrectomy contribute to sustained improvements in glucose control

(2019) Jonathan D. Douros et al.   Molecular Metabolism

Glucose-Dependent Insulinotropic Polypeptide Receptor-Expressing Cells in the Hypothalamus Regulate Food Intake

(2019) Alice E. Adriaenssens et al.   Cell Metabolism

Selection and progression of unimolecular agonists at the GIP, GLP-1, and glucagon receptors as drug candidates

(2019) Patrick J. Knerr 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

GIP’s effect on bone metabolism is reduced by the selective GIP receptor antagonist GIP(3–30)NH2

(2019) Lærke S. Gasbjerg et al.   BONE

Human GIP(3-30)NH 2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors

(2018) Maria Buur Nordskov Gabe et al.   BIOCHEMICAL PHARMACOLOGY

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

Optimized GIP analogs promote body weight lowering in mice through GIPR agonism not antagonism

(2018) Piotr A. Mroz et al.   Molecular Metabolism

N-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptor

(2016) L S Hansen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Species-specific action of (Pro3)GIP - a full agonist at human GIP receptors, but a partial agonist and competitive antagonist at rat and mouse GIP receptors

(2015) A H Sparre-Ulrich et al.   BRITISH JOURNAL OF PHARMACOLOGY

Sequential induction of beta cell rest and stimulation using stable GIP inhibitor and GLP-1 mimetic peptides improves metabolic control in C57BL/KsJ db/db mice

(2015) Varun Pathak et al.   DIABETOLOGIA

Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide

(2015) Jesper Lau et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antagonism of gastric inhibitory polypeptide (GIP) by palmitoylation of GIP analogues with N- and C-terminal modifications improves obesity and metabolic control in high fat fed mice

(2015) V. Pathak et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

TCF1 links GIPR signaling to the control of beta cell function and survival

(2015) Jonathan E Campbell et al.   NATURE MEDICINE

Incretin actions beyond the pancreas: lessons from knockout mice

(2013) Daisuke Yabe et al.   CURRENT OPINION IN PHARMACOLOGY

Characterization and biological actions of N-terminal truncated forms of glucose-dependent insulinotropic polypeptide

(2010) Barry D. Kerr et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Glucagon-Like Peptide-1 Receptor Knockout Mice Are Protected from High-Fat Diet-Induced Insulin Resistance

(2010) Julio E. Ayala et al.   ENDOCRINOLOGY

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