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 …

Fluorescence/bioluminescence resonance energy transfer techniques to study G-protein-coupled receptor activation and signaling

MJ Lohse, S Nuber, C Hoffmann - Pharmacological reviews, 2012 - ASPET
Fluorescence and bioluminescence resonance energy transfer (FRET and BRET)
techniques allow the sensitive monitoring of distances between two labels at the nanometer …

The Concise Guide to PHARMACOLOGY 2013/14: G protein‐coupled receptors

SPH Alexander, HE Benson… - British journal of …, 2013 - Wiley Online Library
Abstract The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …

Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs

C Avet, A Mancini, B Breton, C Le Gouill, AS Hauser… - Elife, 2022 - elifesciences.org
The recognition that individual GPCRs can activate multiple signaling pathways has raised
the possibility of developing drugs selectively targeting therapeutically relevant ones. This …

Recurrent activating mutations of G-protein-coupled receptor CYSLTR2 in uveal melanoma

AR Moore, E Ceraudo, JJ Sher, Y Guan… - Nature …, 2016 - nature.com
Uveal melanomas are molecularly distinct from cutaneous melanomas and lack mutations in
BRAF, NRAS, KIT, and NF1. Instead, they are characterized by activating mutations in GNAQ …

[HTML][HTML] 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 …

The prostanoid EP4 receptor and its signaling pathway

U Yokoyama, K Iwatsubo, M Umemura, T Fujita… - Pharmacological …, 2013 - ASPET
The EP4 prostanoid receptor is one of four receptor subtypes for prostaglandin E2. It
belongs to the family of G protein–coupled receptors. It was originally identified, similar to …

Bioluminescence resonance energy transfer–based imaging of protein–protein interactions in living cells

H Kobayashi, LP Picard, AM Schönegge, M Bouvier - Nature protocols, 2019 - nature.com
Bioluminescence resonance energy transfer (BRET) is a transfer of energy between a
luminescence donor and a fluorescence acceptor. Because BRET occurs when the distance …

Functional selectivity profiling of the angiotensin II type 1 receptor using pathway-wide BRET signaling sensors

Y Namkung, C LeGouill, S Kumar, Y Cao… - Science …, 2018 - science.org
G protein–coupled receptors (GPCRs) are important therapeutic targets that exhibit
functional selectivity (biased signaling), in which different ligands or receptor variants elicit …

Monomeric and dimeric CXCL12 inhibit metastasis through distinct CXCR4 interactions and signaling pathways

LJ Drury, JJ Ziarek, S Gravel… - Proceedings of the …, 2011 - National Acad Sciences
Chemokines and chemokine receptors are extensively and broadly involved in cancer
metastasis. Previously, we demonstrated that epigenetic silencing of the chemokine …