How ligands illuminate GPCR molecular pharmacology

D Wacker, RC Stevens, BL Roth - Cell, 2017 - cell.com
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …

Aquaporins: important but elusive drug targets

AS Verkman, MO Anderson… - Nature reviews Drug …, 2014 - nature.com
The aquaporins (AQPs) are a family of small, integral membrane proteins that facilitate water
transport across the plasma membranes of cells in response to osmotic gradients. Data from …

GPCR-G protein-β-arrestin super-complex mediates sustained G protein signaling

ARB Thomsen, B Plouffe, TJ Cahill, AK Shukla… - Cell, 2016 - cell.com
Classically, G protein-coupled receptor (GPCR) stimulation promotes G protein signaling at
the plasma membrane, followed by rapid β-arrestin-mediated desensitization and receptor …

Small-molecule modulation of protein homeostasis

GM Burslem, CM Crews - Chemical reviews, 2017 - ACS Publications
Control of protein levels by nucleic-acid-based technologies has proven to be a useful
research tool but lacks the advantages of small molecules with respect to cell permeability …

Folding and misfolding of human membrane proteins in health and disease: from single molecules to cellular proteostasis

JT Marinko, H Huang, WD Penn, JA Capra… - Chemical …, 2019 - ACS Publications
Advances over the past 25 years have revealed much about how the structural properties of
membranes and associated proteins are linked to the thermodynamics and kinetics of …

Diabetes insipidus

M Christ-Crain, DG Bichet, WK Fenske… - Nature reviews Disease …, 2019 - nature.com
Diabetes insipidus (DI) is a disorder characterized by excretion of large amounts of
hypotonic urine. Central DI results from a deficiency of the hormone arginine vasopressin …

Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET

Y Namkung, C Le Gouill, V Lukashova… - Nature …, 2016 - nature.com
Endocytosis and intracellular trafficking of receptors are pivotal to maintain physiological
functions and drug action; however, robust quantitative approaches are lacking to study …

Cell death and endoplasmic reticulum stress: disease relevance and therapeutic opportunities

I Kim, W Xu, JC Reed - Nature reviews Drug discovery, 2008 - nature.com
The accumulation of unfolded proteins in the endoplasmic reticulum (ER) represents a
cellular stress induced by multiple stimuli and pathological conditions. These include …

Quality control in the endoplasmic reticulum

L Ellgaard, A Helenius - Nature reviews Molecular cell biology, 2003 - nature.com
The endoplasmic reticulum (ER) has a quality-control system for'proof-reading'newly
synthesized proteins, so that only native conformers reach their final destinations. Non …

Pathophysiology, diagnosis and management of nephrogenic diabetes insipidus

D Bockenhauer, DG Bichet - Nature Reviews Nephrology, 2015 - nature.com
Healthy kidneys maintain fluid and electrolyte homoeostasis by adjusting urine volume and
composition according to physiological needs. The final urine composition is determined in …