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 …

[HTML][HTML] GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics

SC Wright, A Motso, S Koutsilieri, CM Beusch… - Nature …, 2023 - nature.com
G protein-coupled receptors are important drug targets that engage and activate signaling
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

J Lu, SJ Piper, P Zhao, LJ Miller, D Wootten… - International journal of …, 2022 - mdpi.com
Pituitary Adenylate Cyclase-Activating Peptide (PACAP) and Vasoactive Intestinal Peptide
(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 …

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 …

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 …

Structure and Molecular Mechanism of Signaling for the Glucagon-like Peptide-1 Receptor Bound to Gs Protein and Exendin-P5 Biased Agonist

B Li, K Maruszko, SK Kim, MY Yang… - Journal of the …, 2023 - ACS Publications
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 …

Structural and functional diversity among agonist-bound states of the GLP-1 receptor

BP Cary, G Deganutti, P Zhao, TT Truong… - Nature chemical …, 2022 - nature.com
Recent advances in G-protein-coupled receptor (GPCR) structural elucidation have
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 …

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 …