DREADDs for neuroscientists

BL Roth - Neuron, 2016 - cell.com
To understand brain function, it is essential that we discover how cellular signaling specifies
normal and pathological brain function. In this regard, chemogenetic technologies represent …

The structure and function of G-protein-coupled receptors

DM Rosenbaum, SGF Rasmussen, BK Kobilka - Nature, 2009 - nature.com
G-protein-coupled receptors (GPCRs) mediate most of our physiological responses to
hormones, neurotransmitters and environmental stimulants, and so have great potential as …

Structure of a β1-adrenergic G-protein-coupled receptor

T Warne, MJ Serrano-Vega, JG Baker… - Nature, 2008 - nature.com
G-protein-coupled receptors have a major role in transmembrane signalling in most
eukaryotes and many are important drug targets. Here we report the 2.7 Å resolution crystal …

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 …

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 …

A peptide derived from a β2-adrenergic receptor transmembrane domain inhibits both receptor dimerization and activation

TE Hebert, S Moffett, JP Morello, TP Loisel… - Journal of Biological …, 1996 - ASBMB
One of the assumptions of the mobile receptor hypothesis as it relates to G protein-coupled
receptors is that the stoichiometry of receptor, G protein, and effector is 1: 1: 1 (Bourne, HR …

[HTML][HTML] Behavioral stress accelerates prostate cancer development in mice

S Hassan, Y Karpova, D Baiz, D Yancey… - The Journal of …, 2013 - Am Soc Clin Investig
Behavioral stress is known to promote tumor progression in experimental models, but the
role of behavioral stress in cancer initiation is less clear. In this issue, Hassan et al. focus on …

The two-state model of receptor activation

P Leff - Trends in pharmacological sciences, 1995 - cell.com
Over the past few years, the concept that the activation of G protein-coupled receptors and
transmitter-gated ion channels depends on a conformational change has received …

Comparative pharmacology of human β-adrenergic receptor subtypes—characterization of stably transfected receptors in CHO cells

C Hoffmann, MR Leitz, S Oberdorf-Maass… - Naunyn-Schmiedeberg's …, 2004 - Springer
Although many β 1-receptor antagonists and β 2-receptor agonists have been used in
pharmacotherapy for many years their pharmacological properties at all three known …

Multiple ligand-specific conformations of the β2-adrenergic receptor

AW Kahsai, K Xiao, S Rajagopal, S Ahn… - Nature chemical …, 2011 - nature.com
Abstract Seven-transmembrane receptors (7TMRs), also called G protein–coupled receptors
(GPCRs), represent the largest class of drug targets, and they can signal through several …