G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery

M Zhang, T Chen, X Lu, X Lan, Z Chen… - Signal Transduction and …, 2024 - nature.com
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

Glucagon resistance and metabolic-associated steatotic liver disease: a review of the evidence

ER McGlone, SR Bloom… - Journal of Endocrinology, 2024 - joe.bioscientifica.com
Metabolic-associated steatotic liver disease (MASLD) is closely associated with obesity.
MASLD affects over 1 billion adults globally but there are few treatment options available …

ASD2023: towards the integrating landscapes of allosteric knowledgebase

J He, X Liu, C Zhu, J Zha, Q Li, M Zhao… - Nucleic Acids …, 2024 - academic.oup.com
Allosteric regulation, induced by perturbations at an allosteric site topographically distinct
from the orthosteric site, is one of the most direct and efficient ways to fine-tune …

[HTML][HTML] All over or overall–Do we understand allostery?

H Hofmann - Current Opinion in Structural Biology, 2023 - Elsevier
Allostery is probably the most important concept in the regulation of cellular processes.
Models to explain allostery are plenty. Each sheds light on different aspects but their entirety …

Impact of secretin receptor homo-dimerization on natural ligand binding

KG Harikumar, SJ Piper, A Christopoulos… - Nature …, 2024 - nature.com
Class BG protein-coupled receptors can form dimeric complexes important for high potency
biological effects. Here, we apply pharmacological, biochemical, and biophysical techniques …

Single transmembrane GPCR modulating proteins: neither single nor simple

M Wang, J Lyu, C Zhang - Protein & Cell, 2024 - academic.oup.com
The G-protein coupled receptor (GPCR)-mediated signaling participates in almost all known
physiological processes and GPCRs have been validated as a key target family for drug …

[HTML][HTML] Body weight lowering effect of glucose-dependent insulinotropic polypeptide and glucagon-like peptide receptor agonists is more efficient in RAMP1/3 KO …

AS Leuthardt, CN Boyle, K Raun, TA Lutz… - European Journal of …, 2023 - Elsevier
The glucose-dependent insulinotropic polypeptide (GIPR) and glucagon-like peptide (GLP-
1R) receptor agonists are insulin secretagogues that have long been shown to improve …

Glucagon and Its Receptors in the Mammalian Heart

J Neumann, B Hofmann, S Dhein, U Gergs - International Journal of …, 2023 - mdpi.com
Glucagon exerts effects on the mammalian heart. These effects include alterations in the
force of contraction, beating rate, and changes in the cardiac conduction system axis. The …

Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism

J Duan, XH He, SJ Li, HE Xu - Nature Reviews Endocrinology, 2024 - nature.com
G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors, with
many GPCRs having crucial roles in endocrinology and metabolism. Cryogenic electron …

CD9 Counteracts Liver Steatosis and Mediates GCGR Agonist Hepatic Effects

Y Zheng, Y Wang, X Xiong, L Zhang, J Zhu… - Advanced …, 2024 - Wiley Online Library
Glucagon receptor (GCGR) agonism offers potentially greater effects on the mitigation of
hepatic steatosis. However, its underlying mechanism is not fully understood. Here, it …