[HTML][HTML] Advances in therapeutic peptides targeting G protein-coupled receptors
AP Davenport, CCG Scully, C de Graaf… - Nature Reviews Drug …, 2020 - nature.com
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
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 …
Sampling alternative conformational states of transporters and receptors with AlphaFold2
Equilibrium fluctuations and triggered conformational changes often underlie the functional
cycles of membrane proteins. For example, transporters mediate the passage of molecules …
cycles of membrane proteins. For example, transporters mediate the passage of molecules …
[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] Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy
J Duan, D Shen, XE Zhou, P Bi, Q Liu, Y Tan… - Nature …, 2020 - nature.com
Vasoactive intestinal polypeptide receptor (VIP1R) is a widely expressed class BG protein-
coupled receptor and a drug target for the treatment of neuronal, metabolic, and …
coupled receptor and a drug target for the treatment of neuronal, metabolic, and …
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 insights into differences in G protein activation by family A and family B GPCRs
INTRODUCTION Transmembrane signaling of heterotrimeric guanine nucleotide–binding
protein (G protein)–coupled receptors (GPCRs) is mediated by ligand-dependent …
protein (G protein)–coupled receptors (GPCRs) is mediated by ligand-dependent …
[HTML][HTML] Differential GLP-1R binding and activation by peptide and non-peptide agonists
Peptide drugs targeting class B1 G-protein-coupled receptors (GPCRs) can treat multiple
diseases; however, there remains substantial interest in the development of orally delivered …
diseases; however, there remains substantial interest in the development of orally delivered …
[HTML][HTML] β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells
Abstract β-arrestins mediate regulatory processes for over 800 different G protein-coupled
receptors (GPCRs) by adopting specific conformations that result from the geometry of the …
receptors (GPCRs) by adopting specific conformations that result from the geometry of the …