[HTML][HTML] 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 …

Treatment of type 2 diabetes: challenges, hopes, and anticipated successes

MA Nauck, J Wefers, JJ Meier - The lancet Diabetes & endocrinology, 2021 - thelancet.com
Despite the successful development of new therapies for the treatment of type 2 diabetes,
such as glucagon-like peptide-1 (GLP-1) receptor agonists and sodium-glucose …

[HTML][HTML] Receptor-associated independent cAMP nanodomains mediate spatiotemporal specificity of GPCR signaling

SE Anton, C Kayser, I Maiellaro, K Nemec, J Möller… - Cell, 2022 - cell.com
G protein-coupled receptors (GPCRs) relay extracellular stimuli into specific cellular
functions. Cells express many different GPCRs, but all these GPCRs signal to only a few …

[HTML][HTML] Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

FS Willard, JD Douros, MBN Gabe, AD Showalter… - JCI insight, 2020 - ncbi.nlm.nih.gov
Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for
the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis …

[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 …

Dynamic omnidirectional adhesive microneedle system for oral macromolecular drug delivery

W Chen, J Wainer, SW Ryoo, X Qi, R Chang, J Li… - Science …, 2022 - science.org
Oral drug administration remains the preferred route for patients and health care providers.
Delivery of macromolecules through this route remains challenging because of limitations …

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 …

[HTML][HTML] Differential GLP-1R binding and activation by peptide and non-peptide agonists

X Zhang, MJ Belousoff, P Zhao, AJ Kooistra, TT Truong… - Molecular Cell, 2020 - cell.com
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 …

Membranes under the magnetic lens: a dive into the diverse world of membrane protein structures using Cryo-EM

SJ Piper, RM Johnson, D Wootten, PM Sexton - Chemical reviews, 2022 - ACS Publications
Membrane proteins are highly diverse in both structure and function and can, therefore,
present different challenges for structure determination. They are biologically important for …

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 …