The discovery and development of liraglutide and semaglutide

LB Knudsen, J Lau - Frontiers in endocrinology, 2019 - frontiersin.org
The discovery of glucagon-like peptide-1 (GLP-1), an incretin hormone with important effects
on glycemic control and body weight regulation, led to efforts to extend its half-life and make …

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 - Elsevier
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 …

Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein

Y Zhang, B Sun, D Feng, H Hu, M Chu, Q Qu… - Nature, 2017 - nature.com
Abstract Glucagon-like peptide 1 (GLP-1) is a hormone with essential roles in regulating
insulin secretion, carbohydrate metabolism and appetite. GLP-1 effects are mediated …

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex

YL Liang, M Khoshouei, A Glukhova, SGB Furness… - Nature, 2018 - nature.com
The class B glucagon-like peptide-1 (GLP-1) G protein-coupled receptor is a major target for
the treatment of type 2 diabetes and obesity. Endogenous and mimetic GLP-1 peptides …

Differential GLP-1R binding and activation by peptide and non-peptide agonists

X Zhang, MJ Belousoff, P Zhao, AJ Kooistra, TT Truong… - Molecular Cell, 2020 - cell.com
Peptide drugs targeting class B1 G-protein-coupled receptors (GPCRs) can treat multiple
diseases; however, there remains substantial interest in the development of orally delivered …

Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators

G Song, D Yang, Y Wang, C De Graaf, Q Zhou, S Jiang… - Nature, 2017 - nature.com
The glucagon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR) are
members of the secretin-like class B family of G-protein-coupled receptors (GPCRs) and …

Crystal structure of the GLP-1 receptor bound to a peptide agonist

A Jazayeri, M Rappas, AJH Brown, J Kean, JC Errey… - Nature, 2017 - nature.com
Abstract Glucagon-like peptide 1 (GLP-1) regulates glucose homeostasis through the control
of insulin release from the pancreas. GLP-1 peptide agonists are efficacious drugs for the …

Full-length human GLP-1 receptor structure without orthosteric ligands

F Wu, L Yang, K Hang, M Laursen, L Wu… - Nature …, 2020 - nature.com
Abstract Glucagon-like peptide-1 receptor (GLP-1R) is a class BG protein-coupled receptor
that plays an important role in glucose homeostasis and treatment of type 2 diabetes …

Extending the structural view of class B GPCRs

C de Graaf, G Song, C Cao, Q Zhao, MW Wang… - Trends in biochemical …, 2017 - cell.com
The secretin-like class B family of G protein-coupled receptors (GPCRs) are key players in
hormonal homeostasis. Recent structures of various receptors in complex with a variety of …

Structure of the glucagon receptor in complex with a glucagon analogue

H Zhang, A Qiao, L Yang, N Van Eps, KS Frederiksen… - Nature, 2018 - nature.com
Class B G-protein-coupled receptors (GPCRs), which consist of an extracellular domain
(ECD) and a transmembrane domain (TMD), respond to secretin peptides to play a key part …