The GPCR Network: a large-scale collaboration to determine human GPCR structure and function

RC Stevens, V Cherezov, V Katritch… - Nature reviews Drug …, 2013 - nature.com
G protein-coupled receptors (GPCRs) are targeted by∼ 30–40% of marketed drugs, and
their key roles in normal physiology and in disease demonstrate that an understanding of …

An online resource for GPCR structure determination and analysis

C Munk, E Mutt, V Isberg, LF Nikolajsen, JM Bibbe… - Nature …, 2019 - nature.com
G-protein-coupled receptors (GPCRs) transduce physiological and sensory stimuli into
appropriate cellular responses and mediate the actions of one-third of drugs. GPCR …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

Structural insights into the lipid and ligand regulation of serotonin receptors

P Xu, S Huang, H Zhang, C Mao, XE Zhou, X Cheng… - Nature, 2021 - nature.com
Abstract Serotonin, or 5-hydroxytryptamine (5-HT), is an important neurotransmitter, that
activates the largest subtype family of G-protein-coupled receptors. Drugs that target 5 …

Structural basis for strychnine activation of human bitter taste receptor TAS2R46

W Xu, L Wu, S Liu, X Liu, X Cao, C Zhou, J Zhang, Y Fu… - Science, 2022 - science.org
Taste sensing is a sophisticated chemosensory process, and bitter taste perception is
mediated by type 2 taste receptors (TAS2Rs), or class TG protein–coupled receptors …

[HTML][HTML] Crystal structure of an LSD-bound human serotonin receptor

D Wacker, S Wang, JD McCorvy, RM Betz… - Cell, 2017 - cell.com
The prototypical hallucinogen LSD acts via serotonin receptors, and here we describe the
crystal structure of LSD in complex with the human serotonin receptor 5-HT 2B. The complex …

PtdIns (4, 5) P2 stabilizes active states of GPCRs and enhances selectivity of G-protein coupling

HY Yen, KK Hoi, I Liko, G Hedger, MR Horrell, W Song… - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are involved in many physiological processes and are
therefore key drug targets 1. Although detailed structural information is available for GPCRs …

Structural features for functional selectivity at serotonin receptors

D Wacker, C Wang, V Katritch, GW Han, XP Huang… - Science, 2013 - science.org
Drugs active at G protein–coupled receptors (GPCRs) can differentially modulate either
canonical or noncanonical signaling pathways via a phenomenon known as functional …

Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists

B Wu, EYT Chien, CD Mol, G Fenalti, W Liu, V Katritch… - Science, 2010 - science.org
Chemokine receptors are critical regulators of cell migration in the context of immune
surveillance, inflammation, and development. The G protein–coupled chemokine receptor …

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) …