The GPCR Network: a large-scale collaboration to determine human GPCR structure and function
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 …
their key roles in normal physiology and in disease demonstrate that an understanding of …
An online resource for GPCR structure determination and analysis
G-protein-coupled receptors (GPCRs) transduce physiological and sensory stimuli into
appropriate cellular responses and mediate the actions of one-third of drugs. GPCR …
appropriate cellular responses and mediate the actions of one-third of drugs. GPCR …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
Structural insights into the lipid and ligand regulation of serotonin receptors
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 …
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 …
mediated by type 2 taste receptors (TAS2Rs), or class TG protein–coupled receptors …
[HTML][HTML] Crystal structure of an LSD-bound human serotonin receptor
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 …
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
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 …
therefore key drug targets 1. Although detailed structural information is available for GPCRs …
Structural features for functional selectivity at serotonin receptors
Drugs active at G protein–coupled receptors (GPCRs) can differentially modulate either
canonical or noncanonical signaling pathways via a phenomenon known as functional …
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 …
surveillance, inflammation, and development. The G protein–coupled chemokine receptor …
Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism
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) …
egress from the lymph node and an established drug target for multiple sclerosis (MS) …