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 …

New insights in cannabinoid receptor structure and signaling

L Ye, Z Cao, W Wang, N Zhou - Current molecular …, 2019 - ingentaconnect.com
Background: Cannabinoid has long been used for medicinal purposes. Cannabinoid
signaling has been considered the therapeutic target for treating pain, addiction, obesity …

Structure of the µ-opioid receptor–Gi protein complex

A Koehl, H Hu, S Maeda, Y Zhang, Q Qu, JM Paggi… - Nature, 2018 - nature.com
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most
clinically and recreationally used opioids. The induced positive effects of analgesia and …

[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs

A Inoue, F Raimondi, FMN Kadji, G Singh, T Kishi… - Cell, 2019 - cell.com
Heterotrimetic G proteins consist of four subfamilies (G s, G i/o, G q/11, and G 12/13) that
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …

GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors

S Huang, P Xu, DD Shen, IA Simon, C Mao, Y Tan… - Molecular cell, 2022 - cell.com
Summary Serotonin (or 5-hydroxytryptamine, 5-HT) is an important neurotransmitter that
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …

Cryo-EM structure of the serotonin 5-HT1B receptor coupled to heterotrimeric Go

J García-Nafría, R Nehmé, PC Edwards, CG Tate - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) form the largest family of receptors encoded by the
human genome (around 800 genes). They transduce signals by coupling to a small number …

Structural basis of ligand recognition at the human MT1 melatonin receptor

B Stauch, LC Johansson, JD McCorvy, N Patel… - Nature, 2019 - nature.com
Abstract Melatonin (N-acetyl-5-methoxytryptamine) is a neurohormone that maintains
circadian rhythms by synchronization to environmental cues and is involved in diverse …

Adhesion G protein-coupled receptors: opportunities for drug discovery

F Bassilana, M Nash, MG Ludwig - Nature reviews Drug discovery, 2019 - nature.com
Adhesion G protein-coupled receptors (aGPCRs)—one of the five main families in the GPCR
superfamily—have several atypical characteristics, including large, multi-domain N termini …

Engineering cell sensing and responses using a GPCR-coupled CRISPR-Cas system

NH Kipniss, PCDP Dingal, TR Abbott, Y Gao… - Nature …, 2017 - nature.com
G-protein-coupled receptors (GPCRs) are the largest and most diverse group of membrane
receptors in eukaryotes and detect a wide array of cues in the human body. Here we …

Computational design of G Protein-Coupled Receptor allosteric signal transductions

KYM Chen, D Keri, P Barth - Nature Chemical Biology, 2020 - nature.com
Membrane receptors sense and transduce extracellular stimuli into intracellular signaling
responses but the molecular underpinnings remain poorly understood. We report a …