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 …

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 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 …

Elucidating the interactome of G protein-coupled receptors and receptor activity-modifying proteins

IB Kotliar, E Lorenzen, JM Schwenk, DL Hay… - Pharmacological …, 2023 - ASPET
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 …

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 …

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 …

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 …

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 …

Evolving cryo-EM structural approaches for GPCR drug discovery

X Zhang, RM Johnson, I Drulyte, L Yu, A Kotecha… - Structure, 2021 - cell.com
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 …

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 …