GIP as a therapeutic target in diabetes and obesity: insight from incretin co-agonists

JJ Holst, MM Rosenkilde - The Journal of Clinical Endocrinology …, 2020 - academic.oup.com
The 2 hormones responsible for the amplification of insulin secretion after oral as opposed
to intravenous nutrient administration are the gut peptides, glucagon-like peptide-1 (GLP-1) …

[HTML][HTML] Biased agonism and polymorphic variation at the GLP-1 receptor: Implications for the development of personalised therapeutics

L El Eid, CA Reynolds, A Tomas, B Jones - Pharmacological Research, 2022 - Elsevier
Abstract Glucagon-like peptide-1 receptor (GLP-1R) is a well-studied incretin hormone
receptor and target of several therapeutic drugs for type 2 diabetes (T2D), obesity and, more …

Genetic and biased agonist-mediated reductions in β-arrestin recruitment prolong cAMP signaling at glucagon family receptors

B Jones, ER McGlone, Z Fang, P Pickford… - Journal of Biological …, 2021 - ASBMB
Receptors for the peptide hormones glucagon-like peptide-1 (GLP-1R), glucose-dependent
insulinotropic polypeptide (GIPR), and glucagon (GCGR) are important regulators of insulin …

Appetite control: hormones or diet strategies?

RH Freire, JI Alvarez-Leite - Current Opinion in Clinical Nutrition & …, 2020 - journals.lww.com
Appetite control has been an important target for the treatment of obesity and associated
disorders. New studies have demonstrated promising adoption of dietary approaches …

Investigational and emerging gastric inhibitory polypeptide (GIP) receptor-based therapies for the treatment of obesity

RH Gaffey, AK Takyi, A Shukla - Expert Opinion on Investigational …, 2024 - Taylor & Francis
Introduction One billion people live with obesity. The most promising medications for its
treatment are incretin-based therapies, based on enteroendocrine peptides released in …

Differential effects of glucose‐dependent insulinotropic polypeptide receptor/glucagon‐like peptide‐1 receptor heteromerization on cell signaling when expressed in …

B Al‐Zaid, S Chacko, CI Ezeamuzie… - Pharmacology …, 2022 - Wiley Online Library
The incretin hormones: glucose‐dependent insulinotropic polypeptide (GIP) and glucagon‐
like peptide‐1 (GLP‐1) are important regulators of many aspects of metabolism including …

Effects on pancreatic Beta and other Islet cells of the glucose-dependent insulinotropic polypeptide

R Khan, A Tomas, GA Rutter - Peptides, 2020 - Elsevier
Glucose-dependent insulinotropic polypeptide (GIP) is a gut-derived incretin that, in
common with glucagon-like peptide-1 (GLP-1), has both insulin releasing and extra …

Aging-related modifications to G protein-coupled receptor signaling diversity

J van Gastel, H Leysen, J Boddaert, LM Luttrell… - Pharmacology & …, 2021 - Elsevier
Aging is a highly complex molecular process, affecting nearly all tissue systems in humans
and is the highest risk factor in developing neurodegenerative disorders such as Alzheimer's …

Looking ahead to potential incretin combination therapies for nonalcoholic steatohepatitis in patients with diabetes

L Brodosi, ML Petroni, G Marchesini - Expert Opinion on …, 2023 - Taylor & Francis
Introduction There are no drugs approved by regulatory agencies for the treatment of
nonalcoholic fatty liver disease (NAFLD); incretin combination therapies are being …

Improved Split TEV GPCR β-arrestin-2 Recruitment Assays via Systematic Analysis of Signal Peptide and β-arrestin Binding Motif Variants

Y Wu, IV von Hauff, N Jensen, MJ Rossner, MC Wehr - Biosensors, 2022 - mdpi.com
G protein-coupled receptors (GPCRs) are major disease-relevant drug targets; robust
monitoring of their activities upon drug treatment is key to drug discovery. The split TEV cell …