Ligand binding and micro-switches in 7TM receptor structures

R Nygaard, TM Frimurer, B Holst… - Trends in …, 2009 - cell.com
The past couple of years have seen several novel X-ray structures of 7 transmembrane
(7TM) receptors in complex with antagonists and even with a peptide fragment of a G …

Unifying family A GPCR theories of activation

BG Tehan, A Bortolato, FE Blaney, MP Weir… - Pharmacology & …, 2014 - Elsevier
Several new pairs of active and inactive GPCR structures have recently been solved
enabling detailed structural insight into the activation process, not only of rhodopsin but now …

Hormone-and antibody-mediated activation of the thyrotropin receptor

J Duan, P Xu, X Luan, Y Ji, X He, N Song, Q Yuan… - Nature, 2022 - nature.com
Abstract Thyroid-stimulating hormone (TSH), through activation of its G-protein-coupled
thyrotropin receptor (TSHR), controls the synthesis of thyroid hormone—an essential …

Crystal structure of squid rhodopsin

M Murakami, T Kouyama - Nature, 2008 - nature.com
Invertebrate phototransduction uses an inositol-1, 4, 5-trisphosphate signalling cascade in
which photoactivated rhodopsin stimulates a Gq-type G protein, that is, a class of G protein …

Allosteric communication between protomers of dopamine class A GPCR dimers modulates activation

Y Han, IS Moreira, E Urizar, H Weinstein… - Nature chemical …, 2009 - nature.com
A major obstacle to understanding the functional importance of dimerization between class
AG protein–coupled receptors (GPCRs) has been the methodological limitation in achieving …

A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors 2

B Holst, R Nygaard, L Valentin-Hansen, A Bach… - Journal of Biological …, 2010 - jbc.org
The conserved tryptophan in position 13 of TM-VI (Trp-VI: 13 or Trp-6.48) of the CWXP motif
located at the bottom of the main ligand-binding pocket in TM-VI is believed to function as a …

Novel insights on thyroid-stimulating hormone receptor signal transduction

G Kleinau, S Neumann, A Grüters, H Krude… - Endocrine …, 2013 - academic.oup.com
The TSH receptor (TSHR) is a member of the glycoprotein hormone receptors, a subfamily of
family AG protein-coupled receptors. The TSHR is of great importance for the growth and …

Structural–functional features of the thyrotropin receptor: a class A G-protein-coupled receptor at work

G Kleinau, CL Worth, A Kreuchwig… - Frontiers in …, 2017 - frontiersin.org
The thyroid-stimulating hormone receptor (TSHR) is a member of the glycoprotein hormone
receptors, a sub-group of class A G-protein-coupled receptors (GPCRs). TSHR and its …

Pharmacogenomic and structural analysis of constitutive G protein–coupled receptor activity

MJ Smit, HF Vischer, RA Bakker… - Annu. Rev …, 2007 - annualreviews.org
G protein–coupled receptors (GPCRs) respond to a chemically diverse plethora of signal
transduction molecules. The notion that GPCRs also signal without an external chemical …

[HTML][HTML] Thermostabilisation of an agonist-bound conformation of the human adenosine A2A receptor

G Lebon, K Bennett, A Jazayeri, CG Tate - Journal of molecular biology, 2011 - Elsevier
The adenosine A 2A receptor (A 2A R) is a G-protein-coupled receptor that plays a key role
in transmembrane signalling mediated by the agonist adenosine. The structure of A 2A R …