[HTML][HTML] Glucagon-like peptide 1 (GLP-1)

TD Müller, B Finan, SR Bloom, D D'Alessio… - Molecular …, 2019 - Elsevier
Background The glucagon-like peptide-1 (GLP-1) is a multifaceted hormone with broad
pharmacological potential. Among the numerous metabolic effects of GLP-1 are the glucose …

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 …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

Mechanisms of signalling and biased agonism in G protein-coupled receptors

D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

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 class B GPCR–G-protein complex

YL Liang, M Khoshouei, M Radjainia, Y Zhang… - Nature, 2017 - nature.com
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases,
such as osteoporosis, diabetes and obesity. Here we report the structure of a full-length …

[HTML][HTML] Crystal structure of an LSD-bound human serotonin receptor

D Wacker, S Wang, JD McCorvy, RM Betz… - Cell, 2017 - cell.com
The prototypical hallucinogen LSD acts via serotonin receptors, and here we describe the
crystal structure of LSD in complex with the human serotonin receptor 5-HT 2B. The complex …

Advances in therapeutic peptides targeting G protein-coupled receptors

AP Davenport, CCG Scully, C de Graaf… - Nature Reviews Drug …, 2020 - nature.com
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …

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 …