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 …

Insights into the structure of class B GPCRs

K Hollenstein, C de Graaf, A Bortolato… - Trends in …, 2014 - cell.com
The secretin-like (class B) family of G protein-coupled receptors (GPCRs) are key players in
hormonal homeostasis and are interesting drug targets for the treatment of several metabolic …

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 …

Structure of the human glucagon class B G-protein-coupled receptor

FY Siu, M He, C De Graaf, GW Han, D Yang, Z Zhang… - Nature, 2013 - nature.com
Binding of the glucagon peptide to the glucagon receptor (GCGR) triggers the release of
glucose from the liver during fasting; thus GCGR plays an important role in glucose …

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 …

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 …

[HTML][HTML] Gut-brain connection: The neuroprotective effects of the anti-diabetic drug liraglutide

EM Candeias, IC Sebastião, SM Cardoso… - World journal of …, 2015 - ncbi.nlm.nih.gov
Long-acting glucagon-like peptide-1 (GLP-1) analogues marketed for type 2 diabetes (T2D)
treatment have been showing positive and protective effects in several different tissues …

Naturally occurring mutations in G protein-coupled receptors associated with obesity and type 2 diabetes mellitus

T Liu, RL Ji, YX Tao - Pharmacology & Therapeutics, 2022 - Elsevier
G protein-coupled receptors (GPCRs) are the largest family of membrane receptors involved
in the regulation of almost all known physiological processes. Dysfunctions of GPCR …

Transmembrane signal transduction by peptide hormones via family BG protein-coupled receptors

KJ Culhane, Y Liu, Y Cai, ECY Yan - Frontiers in pharmacology, 2015 - frontiersin.org
Although family BG protein-coupled receptors (GPCRs) contain only 15 members, they play
key roles in transmembrane signal transduction of hormones. Family B GPCRs are drug …