A review of current trends with type 2 diabetes epidemiology, aetiology, pathogenesis, treatments and future perspectives

J Reed, S Bain, V Kanamarlapudi - Diabetes, Metabolic Syndrome …, 2021 - Taylor & Francis
Abstract Type 2 diabetes (T2D), which has currently become a global pandemic, is a
metabolic disease largely characterised by impaired insulin secretion and action. Significant …

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 …

[HTML][HTML] Glucagon-like peptide 1 (GLP-1)

TD Müller, B Finan, SR Bloom, D D'Alessio… - Molecular …, 2019 - Elsevier
Background The glucagon-like peptide-1 (GLP-1) is a multifaceted hormone with broad
pharmacological potential. Among the numerous metabolic effects of GLP-1 are the glucose …

Mechanisms of action and therapeutic application of glucagon-like peptide-1

DJ Drucker - Cell metabolism, 2018 - cell.com
Glucagon-like peptide-1 (GLP-1) released from gut enteroendocrine cells controls meal-
related glycemic excursions through augmentation of insulin and inhibition of glucagon …

Mechanisms of signalling and biased agonism in G protein-coupled receptors

D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …

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 …

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 …

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 …

Structural insights into G-protein-coupled receptor allostery

DM Thal, A Glukhova, PM Sexton, A Christopoulos - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …

The pocketome of G-protein-coupled receptors reveals previously untargeted allosteric sites

JB Hedderich, M Persechino, K Becker… - Nature …, 2022 - nature.com
G-protein-coupled receptors do not only feature the orthosteric pockets, where most
endogenous agonists bind, but also a multitude of other allosteric pockets that have come …