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 …

GPCR Engineering Yields High-Resolution Structural Insights into β2-Adrenergic Receptor Function

DM Rosenbaum, V Cherezov, MA Hanson… - science, 2007 - science.org
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 …

Biased Signaling Pathways in β2-Adrenergic Receptor Characterized by 19F-NMR

JJ Liu, R Horst, V Katritch, RC Stevens, K Wüthrich - Science, 2012 - science.org
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 …

[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 …

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 …

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 …

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 - ASBMB
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 …

G protein-coupled receptors: II. Mechanism of agonist activation

U Gether, BK Kobilka - Journal of Biological Chemistry, 1998 - ASBMB
The majority of transmembrane signal transduction in response to hormones and
neurotransmitters is mediated by G proteincoupled receptors (GPCRs). 1 Moreover, GPCRs …

Advances in Determination of a High-Resolution Three-Dimensional Structure of Rhodopsin, a Model of G-Protein-Coupled Receptors (GPCRs),

DC Teller, T Okada, CA Behnke, K Palczewski… - Biochemistry, 2001 - ACS Publications
Membrane proteins, encoded by∼ 20% of genes in almost all organisms, including humans,
are critical for cellular communication, electrical and ion balances, structural integrity of the …

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

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