[HTML][HTML] GLP-1 physiology informs the pharmacotherapy of obesity

DJ Drucker - Molecular metabolism, 2022 - Elsevier
Background Glucagon-like peptide-1 receptor agonists (GLP1RA) augment glucose-
dependent insulin release and reduce glucagon secretion and gastric emptying, enabling …

[HTML][HTML] Mechanisms of action and therapeutic application of glucagon-like peptide-1

DJ Drucker - Cell metabolism, 2018 - cell.com
Glucagon-like peptide-1 (GLP-1) released from gut enteroendocrine cells controls meal-
related glycemic excursions through augmentation of insulin and inhibition of glucagon …

[HTML][HTML] 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

T Coskun, KW Sloop, C Loghin, J Alsina-Fernandez… - Molecular …, 2018 - Elsevier
Objective A novel dual GIP and GLP-1 receptor agonist, LY3298176, was developed to
determine whether the metabolic action of GIP adds to the established clinical benefits of …

[HTML][HTML] The expanding incretin universe: from basic biology to clinical translation

DJ Drucker, JJ Holst - Diabetologia, 2023 - Springer
Incretin hormones, principally glucose-dependent insulinotropic polypeptide (GIP) and
glucagon-like peptide-1 (GLP-1), potentiate meal-stimulated insulin secretion through direct …

Revisiting the complexity of GLP-1 action from sites of synthesis to receptor activation

BA McLean, CK Wong, JE Campbell… - Endocrine …, 2021 - academic.oup.com
Abstract Glucagon-like peptide-1 (GLP-1) is produced in gut endocrine cells and in the
brain, and acts through hormonal and neural pathways to regulate islet function, satiety, and …

[HTML][HTML] The incretin co-agonist tirzepatide requires GIPR for hormone secretion from human islets

K El, JD Douros, FS Willard, A Novikoff, A Sargsyan… - Nature …, 2023 - nature.com
The incretins glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide
1 (GLP-1) mediate insulin responses that are proportionate to nutrient intake to facilitate …

A rationally designed monomeric peptide triagonist corrects obesity and diabetes in rodents

B Finan, B Yang, N Ottaway, DL Smiley, T Ma… - Nature medicine, 2015 - nature.com
We report the discovery of a new monomeric peptide that reduces body weight and diabetic
complications in rodent models of obesity by acting as an agonist at three key metabolically …

Glucagon-like peptide-1 and its class BG protein–coupled receptors: a long march to therapeutic successes

C De Graaf, D Donnelly, D Wootten, J Lau… - Pharmacological …, 2016 - ASPET
The glucagon-like peptide (GLP)-1 receptor (GLP-1R) is a class BG protein–coupled
receptor (GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three …

Cardiovascular actions of incretin-based therapies

JR Ussher, DJ Drucker - Circulation research, 2014 - Am Heart Assoc
Glucagon-like peptide-1 receptor (GLP-1R) agonists and dipeptidyl peptidase-4 (DPP-4)
inhibitors represent 2 distinct classes of incretin-based therapies used for the treatment of …

The structure and function of the glucagon‐like peptide‐1 receptor and its ligands

D Donnelly - British journal of pharmacology, 2012 - Wiley Online Library
Glucagon‐like peptide‐1 (7‐36) amide (GLP‐1) is a 30‐residue peptide hormone released
from intestinal L cells following nutrient consumption. It potentiates the glucose‐induced …