International Union of Basic and Clinical Pharmacology. CV. Somatostatin receptors: structure, function, ligands, and new nomenclature

T Günther, G Tulipano, P Dournaud, C Bousquet… - Pharmacological …, 2018 - ASPET
Somatostatin, also known as somatotropin-release inhibitory factor, is a cyclopeptide that
exerts potent inhibitory actions on hormone secretion and neuronal excitability. Its …

Therapeutic targeting of endosomal G-protein-coupled receptors

ARB Thomsen, DD Jensen, GA Hicks… - Trends in pharmacological …, 2018 - cell.com
G-protein-coupled receptors (GPCRs) are conventionally considered to function at the
plasma membrane, where they detect extracellular ligands and activate heterotrimeric G …

The interplay of glucagon-like peptide-1 receptor trafficking and signalling in pancreatic beta cells

A Marzook, A Tomas, B Jones - Frontiers in endocrinology, 2021 - frontiersin.org
The glucagon-like peptide 1 receptor (GLP-1R) is a class BG protein-coupled receptor
(GPCR) which mediates the effects of GLP-1, an incretin hormone secreted primarily from L …

Biased signaling by endogenous opioid peptides

I Gomes, S Sierra, L Lueptow, A Gupta… - Proceedings of the …, 2020 - National Acad Sciences
Opioids, such as morphine and fentanyl, are widely used for the treatment of severe pain;
however, prolonged treatment with these drugs leads to the development of tolerance and …

Location bias: a “hidden variable” in GPCR pharmacology

DS Eiger, C Hicks, J Gardner, U Pham… - Bioessays, 2023 - Wiley Online Library
G protein‐coupled receptors (GPCRs) are the largest family of transmembrane receptors
and primarily signal through two main effector proteins: G proteins and β‐arrestins. Many …

Biased agonism of endogenous opioid peptides at the μ-opioid receptor

GL Thompson, JR Lane, T Coudrat, PM Sexton… - Molecular …, 2015 - ASPET
Biased agonism is having a major impact on modern drug discovery, and describes the
ability of distinct G protein–coupled receptor (GPCR) ligands to activate different cell …

Ligand-specific factors influencing GLP-1 receptor post-endocytic trafficking and degradation in pancreatic beta cells

Z Fang, S Chen, Y Manchanda, S Bitsi… - International Journal of …, 2020 - mdpi.com
The glucagon-like peptide-1 receptor (GLP-1R) is an important regulator of blood glucose
homeostasis. Ligand-specific differences in membrane trafficking of the GLP-1R influence its …

Combination treatments to enhance peptide receptor radionuclide therapy of neuroendocrine tumours

S Adant, GM Shah, JM Beauregard - European journal of nuclear medicine …, 2020 - Springer
The incidence of neuroendocrine tumours (NETs) is increasing, but curative therapeutic
options are limited because diagnosis is often delayed until the tumour has metastasized …

[HTML][HTML] From membrane to nucleus: A three-wave hypothesis of cAMP signaling

A Pizzoni, X Zhang, DL Altschuler - Journal of Biological Chemistry, 2023 - Elsevier
For many decades, our understanding of G protein-coupled receptor (GPCR) activity and
cyclic AMP (cAMP) signaling was limited exclusively to the plasma membrane. However, a …

β-arrestin signalling and bias in hormone-responsive GPCRs

E Reiter, MA Ayoub, LP Pellissier, F Landomiel… - Molecular and Cellular …, 2017 - Elsevier
G protein-coupled receptors (GPCRs) play crucial roles in the ability of target organs to
respond to hormonal cues. GPCRs' activation mechanisms have long been considered as a …