Therapeutic potential of β-arrestin-and G protein-biased agonists

EJ Whalen, S Rajagopal, RJ Lefkowitz - Trends in molecular medicine, 2011 - cell.com
Members of the seven-transmembrane receptor (7TMR), or G protein-coupled receptor
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …

G protein-coupled receptor (GPCR) gene variants and human genetic disease

MD Thompson, ME Percy, DEC Cole… - Critical Reviews in …, 2024 - Taylor & Francis
Genetic variations in the genes encoding G protein-coupled receptors (GPCRs) can disrupt
receptor structure and function, which can result in human genetic diseases. Disease …

CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans

CW White, S Platt, LE Kilpatrick, N Dale… - Science …, 2024 - science.org
CXCL17 is a chemokine principally expressed by mucosal tissues, where it facilitates
chemotaxis of monocytes, dendritic cells, and macrophages and has antimicrobial …

[HTML][HTML] Relaxin requires the angiotensin II type 2 receptor to abrogate renal interstitial fibrosis

BSM Chow, M Kocan, S Bosnyak, M Sarwar, B Wigg… - Kidney international, 2014 - Elsevier
Fibrosis is a hallmark of chronic kidney disease, for which there is currently no effective cure.
The hormone relaxin is emerging as an effective antifibrotic therapy; however, its …

Using nanoBRET and CRISPR/Cas9 to monitor proximity to a genome-edited protein in real-time

CW White, HK Vanyai, HB See, EKM Johnstone… - Scientific Reports, 2017 - nature.com
Bioluminescence resonance energy transfer (BRET) has been a vital tool for understanding
G protein-coupled receptor (GPCR) function. It has been used to investigate GPCR-protein …

The bile acid receptor TGR5 does not interact with β-arrestins or traffic to endosomes but transmits sustained signals from plasma membrane rafts

DD Jensen, CB Godfrey, C Niklas, M Canals… - Journal of Biological …, 2013 - ASBMB
TGR5 is a G protein-coupled receptor that mediates bile acid (BA) effects on energy
balance, inflammation, digestion, and sensation. The mechanisms and spatiotemporal …

The chemokine receptor CCR1 is constitutively active, which leads to G protein-independent, β-arrestin-mediated internalization

CT Gilliland, CL Salanga, T Kawamura, JA Trejo… - Journal of Biological …, 2013 - ASBMB
Activation of G protein-coupled receptors by their associated ligands has been extensively
studied, and increasing structural information about the molecular mechanisms underlying …

[HTML][HTML] Mutation in the V2 vasopressin receptor gene, AVPR2, causes nephrogenic syndrome of inappropriate diuresis

LS Erdélyi, WA Mann, DJ Morris-Rosendahl, U Groß… - Kidney International, 2015 - Elsevier
Nephrogenic syndrome of inappropriate antidiuresis (NSIAD) is a recently discovered rare
disease caused by gain-of-function mutations of the V2 vasopressin receptor gene, AVPR2 …

Mutations of vasopressin receptor 2 including novel L312S have differential effects on trafficking

A Tiulpakov, CW White… - Molecular …, 2016 - academic.oup.com
Nephrogenic syndrome of inappropriate antidiuresis (NSIAD) is a genetic disease first
described in 2 unrelated male infants with severe symptomatic hyponatremia. Despite …

Identification and characterization of an activating F229V substitution in the V2 vasopressin receptor in an infant with NSIAD

E Carpentier, LA Greenbaum, D Rochdi… - Journal of the …, 2012 - journals.lww.com
Gain-of-function mutations in the gene encoding the V2 vasopressin receptor (V2R) cause
nephrogenic syndrome of inappropriate antidiuresis. To date, reported mutations lead to the …