The role of structural dynamics in GPCR‐mediated signaling

D Hilger - The FEBS journal, 2021 - Wiley Online Library
G protein‐coupled receptors (GPCRs) play critical roles in the regulation of human
physiology in response to a wide array of different extracellular stimuli and thus represent …

Lipid nanodiscs for high-resolution NMR studies of membrane proteins

U Günsel, F Hagn - Chemical Reviews, 2021 - ACS Publications
Membrane proteins (MPs) play essential roles in numerous cellular processes. Because
around 70% of the currently marketed drugs target MPs, a detailed understanding of their …

Improved green and red GRAB sensors for monitoring dopaminergic activity in vivo

Y Zhuo, B Luo, X Yi, H Dong, X Miao, J Wan… - Nature …, 2024 - nature.com
Dopamine (DA) plays multiple roles in a wide range of physiological and pathological
processes via a large network of dopaminergic projections. To dissect the spatiotemporal …

[HTML][HTML] Structural insights into the human D1 and D2 dopamine receptor signaling complexes

Y Zhuang, P Xu, C Mao, L Wang, B Krumm, XE Zhou… - Cell, 2021 - cell.com
Summary The D1-and D2-dopamine receptors (D1R and D2R), which signal through G s
and G i, respectively, represent the principal stimulatory and inhibitory dopamine receptors …

[HTML][HTML] Delineating the conformational landscape of the adenosine A2A receptor during G protein coupling

SK Huang, A Pandey, DP Tran, NL Villanueva, A Kitao… - Cell, 2021 - cell.com
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
are important drug targets. Their diverse signaling pathways are driven by complex …

[HTML][HTML] Ligand recognition and allosteric regulation of DRD1-Gs signaling complexes

P Xiao, W Yan, L Gou, YN Zhong, L Kong, C Wu… - Cell, 2021 - cell.com
Dopamine receptors, including D1-and D2-like receptors, are important therapeutic targets
in a variety of neurological syndromes, as well as cardiovascular and kidney diseases. Here …

Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism

Z Xu, T Ikuta, K Kawakami, R Kise, Y Qian… - Nature chemical …, 2022 - nature.com
Abstract Sphingosine-1-phosphate receptor 1 (S1PR1) is a master regulator of lymphocyte
egress from the lymph node and an established drug target for multiple sclerosis (MS) …

[HTML][HTML] Cryo-EM structure of the human histamine H1 receptor/Gq complex

R Xia, N Wang, Z Xu, Y Lu, J Song, A Zhang… - Nature …, 2021 - nature.com
Histamine receptors play important roles in various pathophysiological conditions and are
effective targets for anti-allergy treatment, however the mechanism of receptor activation …

Structure reveals the activation mechanism of the MC4 receptor to initiate satiation signaling

H Israeli, O Degtjarik, F Fierro, V Chunilal, AK Gill… - Science, 2021 - science.org
Obesity is a global epidemic that causes morbidity and impaired quality of life. The
melanocortin receptor 4 (MC4R) is at the crux of appetite, energy homeostasis, and body …

[HTML][HTML] Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling

Y Qian, Z Ma, C Liu, X Li, X Zhu, N Wang, Z Xu, R Xia… - Molecular Cell, 2022 - cell.com
Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of
physiologies. A hallmark of aGPCR activation is the removal of the inhibitory GAIN domain …