New insights into the structure and function of class B1 GPCRs

BP Cary, X Zhang, J Cao, RM Johnson… - Endocrine …, 2023 - academic.oup.com
G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors. Class
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …

Structural perspective of class B1 GPCR signaling

Z Cong, YL Liang, Q Zhou, S Darbalaei, F Zhao… - Trends in …, 2022 - cell.com
Class B1 G protein-coupled receptors (GPCRs) play important roles in human physiology
and disease pathology. Using cryo-electron microscopy (cryo-EM) and X-ray …

Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors

F Zhao, Q Zhou, Z Cong, K Hang, X Zou… - Nature …, 2022 - nature.com
Glucose homeostasis, regulated by glucose-dependent insulinotropic polypeptide (GIP),
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …

Structural analysis of the dual agonism at GLP-1R and GCGR

Y Li, Q Zhou, A Dai, F Zhao, R Chang… - Proceedings of the …, 2023 - National Acad Sciences
Glucagon-like peptide-1 receptor (GLP-1R) and glucagon receptor (GCGR), two members of
class B1 G protein–coupled receptors, play important roles in glucose homeostasis and …

[HTML][HTML] Class B1 GPCR activation by an intracellular agonist

K Kobayashi, K Kawakami, T Kusakizako, A Tomita… - Nature, 2023 - nature.com
G protein-coupled receptors (GPCRs) generally accommodate specific ligands in the
orthosteric-binding pockets. Ligand binding triggers a receptor allosteric conformational …

Allosteric modulation of G protein-coupled receptor signaling

S Shen, C Zhao, C Wu, S Sun, Z Li, W Yan… - Frontiers in …, 2023 - frontiersin.org
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins,
regulate a wide array of physiological processes in response to extracellular signals …

Allosteric modulation of GPCRs: From structural insights to in silico drug discovery

M Persechino, JB Hedderich, P Kolb… - Pharmacology & …, 2022 - Elsevier
G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one of
the prime targets for marketed drugs. While traditional drug discovery programs have …

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 …

[HTML][HTML] Biased agonism and polymorphic variation at the GLP-1 receptor: Implications for the development of personalised therapeutics

L El Eid, CA Reynolds, A Tomas, B Jones - Pharmacological Research, 2022 - Elsevier
Abstract Glucagon-like peptide-1 receptor (GLP-1R) is a well-studied incretin hormone
receptor and target of several therapeutic drugs for type 2 diabetes (T2D), obesity and, more …

Structure, function and drug discovery of GPCR signaling

L Cheng, F Xia, Z Li, C Shen, Z Yang, H Hou… - Molecular …, 2023 - Springer
G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …