Mechanisms of signalling and biased agonism in G protein-coupled receptors
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 …
humans that signal in response to diverse inputs and regulate a plethora of cellular …
Advances in therapeutic peptides targeting G protein-coupled receptors
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein
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 …
insulin secretion, carbohydrate metabolism and appetite. GLP-1 effects are mediated …
Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors
Glucose homeostasis, regulated by glucose-dependent insulinotropic polypeptide (GIP),
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …
Phase-plate cryo-EM structure of a class B GPCR–G-protein complex
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 …
such as osteoporosis, diabetes and obesity. Here we report the structure of a full-length …
Lipidic cubic phase injector facilitates membrane protein serial femtosecond crystallography
Lipidic cubic phase (LCP) crystallization has proven successful for high-resolution structure
determination of challenging membrane proteins. Here we present a technique for extruding …
determination of challenging membrane proteins. Here we present a technique for extruding …
Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy
J Duan, D Shen, XE Zhou, P Bi, Q Liu, Y Tan… - Nature …, 2020 - nature.com
Vasoactive intestinal polypeptide receptor (VIP1R) is a widely expressed class BG protein-
coupled receptor and a drug target for the treatment of neuronal, metabolic, and …
coupled receptor and a drug target for the treatment of neuronal, metabolic, and …
Generic GPCR residue numbers–aligning topology maps while minding the gaps
Generic residue numbers facilitate comparisons of, for example, mutational effects, ligand
interactions, and structural motifs. The numbering scheme by Ballesteros and Weinstein for …
interactions, and structural motifs. The numbering scheme by Ballesteros and Weinstein for …
Glucagon-like peptide-1 and its class BG protein–coupled receptors: a long march to therapeutic successes
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 …
receptor (GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three …
Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex
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 …
the treatment of type 2 diabetes and obesity. Endogenous and mimetic GLP-1 peptides …