G protein-coupled receptors: structure-and function-based drug discovery
D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
New insights into the structure and function of class B1 GPCRs
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 …
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …
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 …
Elucidating the interactome of G protein-coupled receptors and receptor activity-modifying proteins
G protein-coupled receptors (GPCRs) are known to interact with several other classes of
integral membrane proteins that modulate their biology and pharmacology. However, the …
integral membrane proteins that modulate their biology and pharmacology. However, the …
Structural perspective of class B1 GPCR signaling
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 …
and disease pathology. Using cryo-electron microscopy (cryo-EM) and X-ray …
GLP-1 and GLP-2 orchestrate intestine integrity, gut microbiota, and immune system crosstalk
N Abdalqadir, K Adeli - Microorganisms, 2022 - mdpi.com
The intestine represents the body's largest interface between internal organs and external
environments except for its nutrient and fluid absorption functions. It has the ability to sense …
environments except for its nutrient and fluid absorption functions. It has the ability to sense …
Molecular mechanisms of PTH/PTHrP class B GPCR signaling and pharmacological implications
JP Vilardaga, LJ Clark, AD White… - Endocrine …, 2023 - academic.oup.com
The classical paradigm of G protein-coupled receptor (GPCR) signaling via G proteins is
grounded in a view that downstream responses are relatively transient and confined to the …
grounded in a view that downstream responses are relatively transient and confined to the …
Molecular basis for kinin selectivity and activation of the human bradykinin receptors
YL Yin, C Ye, F Zhou, J Wang, D Yang, W Yin… - Nature structural & …, 2021 - nature.com
Bradykinin and kallidin are endogenous kinin peptide hormones that belong to the kallikrein–
kinin system and are essential to the regulation of blood pressure, inflammation, coagulation …
kinin system and are essential to the regulation of blood pressure, inflammation, coagulation …
Evolving cryo-EM structural approaches for GPCR drug discovery
G protein-coupled receptors (GPCRs) are the largest class of cell surface drug targets.
Advances in stabilization of GPCR: transducer complexes, together with improvements in …
Advances in stabilization of GPCR: transducer complexes, together with improvements in …
GIP and GLP-2 together improve bone turnover in humans supporting GIPR-GLP-2R co-agonists as future osteoporosis treatment
MBN Gabe, K Skov-Jeppesen, LS Gasbjerg… - Pharmacological …, 2022 - Elsevier
The intestinal hormones glucose-dependent insulinotropic polypeptide (GIP) and glucagon-
like peptide-2 (GLP-2) are key regulators of postprandial bone turnover in humans. We …
like peptide-2 (GLP-2) are key regulators of postprandial bone turnover in humans. We …