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 …
[HTML][HTML] GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics
G protein-coupled receptors are important drug targets that engage and activate signaling
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
[HTML][HTML] Targeting VIP and PACAP receptor signaling: new insights into designing drugs for the PACAP subfamily of receptors
Pituitary Adenylate Cyclase-Activating Peptide (PACAP) and Vasoactive Intestinal Peptide
(VIP) are neuropeptides involved in a diverse array of physiological and pathological …
(VIP) are neuropeptides involved in a diverse array of physiological and pathological …
Structural determinants of dual incretin receptor agonism by tirzepatide
B Sun, FS Willard, D Feng… - Proceedings of the …, 2022 - National Acad Sciences
Tirzepatide (LY3298176) is a fatty-acid-modified, dual incretin receptor agonist that exhibits
pharmacology similar to native GIP at the glucose-dependent insulinotropic polypeptide …
pharmacology similar to native GIP at the glucose-dependent insulinotropic polypeptide …
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 …
class B1 G protein–coupled receptors, play important roles in glucose homeostasis and …
Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide–Target Interactions
Y Shi, Y Chen, L Deng, K Du, S Lu… - Journal of Medicinal …, 2023 - ACS Publications
The activation of G protein-coupled receptors (GPCRs) is triggered by ligand binding to their
orthosteric sites, which induces ligand-specific conformational changes. Agonists and …
orthosteric sites, which induces ligand-specific conformational changes. Agonists and …
Structure and Molecular Mechanism of Signaling for the Glucagon-like Peptide-1 Receptor Bound to Gs Protein and Exendin-P5 Biased Agonist
The glucagon-like peptide-1 receptor (GLP-1R) is a key regulator of blood glucose and a
prime target for the treatment of type II diabetes and obesity with multiple public drugs. Here …
prime target for the treatment of type II diabetes and obesity with multiple public drugs. Here …
Structural and functional diversity among agonist-bound states of the GLP-1 receptor
Recent advances in G-protein-coupled receptor (GPCR) structural elucidation have
strengthened previous hypotheses that multidimensional signal propagation mediated by …
strengthened previous hypotheses that multidimensional signal propagation mediated by …
[HTML][HTML] Does receptor balance matter?–Comparing the efficacies of the dual amylin and calcitonin receptor agonists cagrilintide and KBP-336 on metabolic …
AT Larsen, KE Mohamed, N Sonne, E Bredtoft… - Biomedicine & …, 2022 - Elsevier
Cagrilintide is a novel long-acting amylin receptor agonist, which has shown a potent
induction of weight loss. Interestingly, cagrilintide is a Dual Amylin and Calcitonin Receptor …
induction of weight loss. Interestingly, cagrilintide is a Dual Amylin and Calcitonin Receptor …
Hormone Analogues with Unique Signaling Profiles from Replacement of α-Residue Triads with β/γ Diads
R Gibadullin, TW Kim, LML Tran… - Journal of the American …, 2023 - ACS Publications
We have applied an underexplored backbone modification strategy to generate new
analogues of peptides that activate two clinically important class B1 G protein-coupled …
analogues of peptides that activate two clinically important class B1 G protein-coupled …