[HTML][HTML] Emerging role of GLP-1 agonists in obesity: a comprehensive review of randomised controlled trials
MS Popoviciu, L Păduraru, G Yahya… - International journal of …, 2023 - mdpi.com
Obesity is a chronic disease with high prevalence and associated comorbidities, making it a
growing global concern. These comorbidities include type 2 diabetes, hypertension …
growing global concern. These comorbidities include type 2 diabetes, hypertension …
Metabolic messengers: glucagon-like peptide 1
FM Gribble, F Reimann - Nature metabolism, 2021 - nature.com
Abstract Glucagon like peptide-1 (GLP-1), a peptide hormone from the intestinal tract, plays
a central role in the coordination of postprandial glucose homeostasis through actions on …
a central role in the coordination of postprandial glucose homeostasis through actions on …
[HTML][HTML] GPCR activation mechanisms across classes and macro/microscales
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
[HTML][HTML] 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 …
[HTML][HTML] De novo design of high-affinity binders of bioactive helical peptides
Many peptide hormones form an α-helix on binding their receptors,,–, and sensitive methods
for their detection could contribute to better clinical management of disease. De novo protein …
for their detection could contribute to better clinical management of disease. De novo protein …
[HTML][HTML] GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors
Summary Serotonin (or 5-hydroxytryptamine, 5-HT) is an important neurotransmitter that
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …
[HTML][HTML] GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics
G protein-coupled receptors are important drug targets that engage and activate signaling
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
Conserved class B GPCR activation by a biased intracellular agonist
LH Zhao, Q He, Q Yuan, Y Gu, X He, H Shan, J Li… - Nature, 2023 - nature.com
Class B G-protein-coupled receptors (GPCRs), including glucagon-like peptide 1 receptor
(GLP1R) and parathyroid hormone 1 receptor (PTH1R), are important drug targets …
(GLP1R) and parathyroid hormone 1 receptor (PTH1R), are important drug targets …
Structural determinants of dual incretin receptor agonism by tirzepatide
B Sun, FS Willard, D Feng… - Proceedings of the …, 2022 - National Acad Sciences
Tirzepatide (LY3298176) is a fatty-acid-modified, dual incretin receptor agonist that exhibits
pharmacology similar to native GIP at the glucose-dependent insulinotropic polypeptide …
pharmacology similar to native GIP at the glucose-dependent insulinotropic polypeptide …
Membranes under the magnetic lens: a dive into the diverse world of membrane protein structures using Cryo-EM
Membrane proteins are highly diverse in both structure and function and can, therefore,
present different challenges for structure determination. They are biologically important for …
present different challenges for structure determination. They are biologically important for …