How ligands illuminate GPCR molecular pharmacology
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 …
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 …
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 …
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 …
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
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 …
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 …
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 …
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 …
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 …
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 …
composition according to physiological needs. The final urine composition is determined in …