G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

Impact of GPCR structures on drug discovery

M Congreve, C de Graaf, NA Swain, CG Tate - Cell, 2020 - cell.com
Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with
over 370 structures in total bound to different ligands and the receptors in various …

Atg9 is a lipid scramblase that mediates autophagosomal membrane expansion

K Matoba, T Kotani, A Tsutsumi, T Tsuji, T Mori… - Nature structural & …, 2020 - nature.com
The molecular function of Atg9, the sole transmembrane protein in the autophagosome-
forming machinery, remains unknown. Atg9 colocalizes with Atg2 at the expanding edge of …

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 …

Structure and gating mechanism of the α7 nicotinic acetylcholine receptor

CM Noviello, A Gharpure, N Mukhtasimova, R Cabuco… - Cell, 2021 - cell.com
The α7 nicotinic acetylcholine receptor plays critical roles in the central nervous system and
in the cholinergic inflammatory pathway. This ligand-gated ion channel assembles as a …

[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 …

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 …

[HTML][HTML] Crystal structure of the human cannabinoid receptor CB2

X Li, T Hua, K Vemuri, JH Ho, Y Wu, L Wu, P Popov… - Cell, 2019 - cell.com
The cannabinoid receptor CB2 is predominately expressed in the immune system, and
selective modulation of CB2 without the psychoactivity of CB1 has therapeutic potential in …

Unsaturated bond recognition leads to biased signal in a fatty acid receptor

C Mao, P Xiao, XN Tao, J Qin, QT He, C Zhang… - Science, 2023 - science.org
Individual free fatty acids (FAs) play important roles in metabolic homeostasis, many through
engagement with more than 40G protein–coupled receptors. Searching for receptors to …

Crystal structures of agonist-bound human cannabinoid receptor CB1

T Hua, K Vemuri, SP Nikas, RB Laprairie, Y Wu, L Qu… - Nature, 2017 - nature.com
Abstract The cannabinoid receptor 1 (CB1) is the principal target of the psychoactive
constituent of marijuana, the partial agonist Δ9-tetrahydrocannabinol (Δ9-THC). Here we …