[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 …
pharmacological potential. Among the numerous metabolic effects of GLP-1 are the glucose …
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 …
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 …
Differential GLP-1R binding and activation by peptide and non-peptide agonists
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 …
diseases; however, there remains substantial interest in the development of orally delivered …
Activation of the GLP-1 receptor by a non-peptidic agonist
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases,
including diabetes and obesity. Structures of active receptors reveal peptide agonists …
including diabetes and obesity. Structures of active receptors reveal peptide agonists …
Human GLP1R variants affecting GLP1R cell surface expression are associated with impaired glucose control and increased adiposity
W Gao, L Liu, E Huh, F Gbahou, E Cecon… - Nature …, 2023 - nature.com
The glucagon-like peptide 1 receptor (GLP1R) is a major drug target with several agonists
being prescribed in individuals with type 2 diabetes and obesity,. The impact of genetic …
being prescribed in individuals with type 2 diabetes and obesity,. The impact of genetic …
Regulation of glucose homeostasis by GLP-1
P Nadkarni, OG Chepurny, GG Holz - Progress in molecular biology and …, 2014 - Elsevier
Abstract Glucagon-like peptide-1 (7–36) amide (GLP-1) is a secreted peptide that acts as a
key determinant of blood glucose homeostasis by virtue of its abilities to slow gastric …
key determinant of blood glucose homeostasis by virtue of its abilities to slow gastric …
A small-molecule oral agonist of the human glucagon-like peptide-1 receptor
DA Griffith, DJ Edmonds, JP Fortin… - Journal of Medicinal …, 2022 - ACS Publications
Peptide agonists of the glucagon-like peptide-1 receptor (GLP-1R) have revolutionized
diabetes therapy, but their use has been limited because they require injection. Herein, we …
diabetes therapy, but their use has been limited because they require injection. Herein, we …
[PDF][PDF] Novel allosteric modulators of G protein-coupled receptors
G protein-coupled receptors (GPCRs) are allosteric proteins, because their signal
transduction relies on interactions between topographically distinct, yet conformationally …
transduction relies on interactions between topographically distinct, yet conformationally …
Practical strategies and concepts in GPCR allosteric modulator discovery: recent advances with metabotropic glutamate receptors
CW Lindsley, KA Emmitte, CR Hopkins… - Chemical …, 2016 - ACS Publications
Allosteric modulation of GPCRs has initiated a new era of basic and translational discovery,
filled with therapeutic promise yet fraught with caveats. Allosteric ligands stabilize unique …
filled with therapeutic promise yet fraught with caveats. Allosteric ligands stabilize unique …