GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures
I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …
physiological processes and thus have long been attractive drug targets. With the crystal …
Functional selectivity and classical concepts of quantitative pharmacology
The concept of intrinsic efficacy has been enshrined in pharmacology for half of a century,
yet recent data have revealed that many ligands can differentially activate signaling …
yet recent data have revealed that many ligands can differentially activate signaling …
Biased Signaling Pathways in β2-Adrenergic Receptor Characterized by 19F-NMR
Extracellular ligand binding to G protein–coupled receptors (GPCRs) modulates G protein
and β-arrestin signaling by changing the conformational states of the cytoplasmic region of …
and β-arrestin signaling by changing the conformational states of the cytoplasmic region of …
GPCR Engineering Yields High-Resolution Structural Insights into β2-Adrenergic Receptor Function
The β2-adrenergic receptor (β2AR) is a well-studied prototype for heterotrimeric guanine
nucleotide–binding protein (G protein)–coupled receptors (GPCRs) that respond to diffusible …
nucleotide–binding protein (G protein)–coupled receptors (GPCRs) that respond to diffusible …
[HTML][HTML] G protein coupled receptor structure and activation
BK Kobilka - Biochimica et Biophysica Acta (BBA)-Biomembranes, 2007 - Elsevier
G protein coupled receptors (GPCRs) are remarkably versatile signaling molecules. The
members of this large family of membrane proteins are activated by a spectrum of …
members of this large family of membrane proteins are activated by a spectrum of …
Uncovering molecular mechanisms involved in activation of G protein-coupled receptors
U Gether - Endocrine reviews, 2000 - academic.oup.com
G protein-coupled, seven-transmembrane segment receptors (GPCRs or 7TM receptors),
with more than 1000 different members, comprise the largest superfamily of proteins in the …
with more than 1000 different members, comprise the largest superfamily of proteins in the …
Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors
R Seifert, K Wenzel-Seifert - Naunyn-Schmiedeberg's archives of …, 2002 - Springer
The aim of this review is to provide a systematic overview on constitutively active G-protein-
coupled receptors (GPCRs), a rapidly evolving area in signal transduction research. We will …
coupled receptors (GPCRs), a rapidly evolving area in signal transduction research. We will …
Fluorescence/bioluminescence resonance energy transfer techniques to study G-protein-coupled receptor activation and signaling
MJ Lohse, S Nuber, C Hoffmann - Pharmacological reviews, 2012 - Elsevier
Fluorescence and bioluminescence resonance energy transfer (FRET and BRET)
techniques allow the sensitive monitoring of distances between two labels at the nanometer …
techniques allow the sensitive monitoring of distances between two labels at the nanometer …
Activation of the β2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6
JA Ballesteros, AD Jensen, G Liapakis… - Journal of Biological …, 2001 - jbc.org
The movements of transmembrane segments (TMs) 3 and 6 at the cytoplasmic side of the
membrane play an important role in the activation of G-protein-coupled receptors. Here we …
membrane play an important role in the activation of G-protein-coupled receptors. Here we …
Methodological advances: the unsung heroes of the GPCR structural revolution
G protein-coupled receptors (GPCRs) are intricately involved in a diverse array of
physiological processes and pathophysiological conditions. They constitute the largest class …
physiological processes and pathophysiological conditions. They constitute the largest class …