Revisiting the complexity of GLP-1 action from sites of synthesis to receptor activation

BA McLean, CK Wong, JE Campbell… - Endocrine …, 2021 - academic.oup.com
Abstract Glucagon-like peptide-1 (GLP-1) is produced in gut endocrine cells and in the
brain, and acts through hormonal and neural pathways to regulate islet function, satiety, and …

β− Arrestins: structure, function, physiology, and pharmacological perspectives

J Wess, AB Oteng, O Rivera-Gonzalez… - Pharmacological …, 2023 - Elsevier
The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …

Pharmacogenomics of GLP-1 receptor agonists: a genome-wide analysis of observational data and large randomised controlled trials

AY Dawed, A Mari, A Brown, TJ McDonald… - The Lancet Diabetes & …, 2023 - thelancet.com
Background In the treatment of type 2 diabetes, GLP-1 receptor agonists lower blood
glucose concentrations, body weight, and have cardiovascular benefits. The efficacy and …

Targeting GLP-1 receptor trafficking to improve agonist efficacy

B Jones, T Buenaventura, N Kanda… - Nature …, 2018 - nature.com
Abstract Glucagon-like peptide-1 receptor (GLP-1R) activation promotes insulin secretion
from pancreatic beta cells, causes weight loss, and is an important pharmacological target in …

The Role of G Protein–Coupled Receptors and Receptor Kinases in Pancreatic β-Cell Function and Diabetes

MJ Varney, JL Benovic, M Michel - Pharmacological reviews, 2024 - Elsevier
Abstract Type 2 diabetes (T2D) mellitus has emerged as a major global health concern that
has accelerated in recent years due to poor diet and lifestyle. Afflicted individuals have high …

PDX1 is the cornerstone of pancreatic β-cell functions and identity

N Ebrahim, K Shakirova… - Frontiers in Molecular …, 2022 - frontiersin.org
Diabetes has been a worldwide healthcare problem for many years. Current methods of
treating diabetes are still largely directed at symptoms, aiming to control the manifestations …

GLP-1 and GIP receptors signal through distinct β-arrestin 2-dependent pathways to regulate pancreatic β cell function

N Zaïmia, J Obeid, A Varrault, J Sabatier, C Broca… - Cell reports, 2023 - cell.com
Summary Glucagon-like peptide 1 (GLP-1R) and glucose-dependent insulinotropic
polypeptide (GIPR) receptors are G-protein-coupled receptors involved in glucose …

A metabolic role for CD47 in pancreatic β cell insulin secretion and islet transplant outcomes

K Ghimire, A Kale, J Li, SM Julovi… - Science Translational …, 2023 - science.org
Diabetes is a global public health burden and is characterized clinically by relative or
absolute insulin deficiency. Therapeutic agents that stimulate insulin secretion and improve …

[HTML][HTML] Intraislet glucagon signaling is critical for maintaining glucose homeostasis

L Zhu, D Dattaroy, J Pham, L Wang, LF Barella, Y Cui… - JCI insight, 2019 - ncbi.nlm.nih.gov
Glucagon, a hormone released from pancreatic α cells, plays a key role in maintaining
proper glucose homeostasis and has been implicated in the pathophysiology of diabetes. In …

Novel metabolic role for BDNF in pancreatic β-cell insulin secretion

G Fulgenzi, Z Hong, F Tomassoni-Ardori… - Nature …, 2020 - nature.com
BDNF signaling in hypothalamic circuitries regulates mammalian food intake. However,
whether BDNF exerts metabolic effects on peripheral organs is currently unknown. Here, we …