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 …

Membranes under the magnetic lens: a dive into the diverse world of membrane protein structures using Cryo-EM

SJ Piper, RM Johnson, D Wootten, PM Sexton - Chemical reviews, 2022 - ACS Publications
Membrane proteins are highly diverse in both structure and function and can, therefore,
present different challenges for structure determination. They are biologically important for …

G-protein activation by a metabotropic glutamate receptor

AB Seven, X Barros-Álvarez, M de Lapeyrière… - Nature, 2021 - nature.com
Family C G-protein-coupled receptors (GPCRs) operate as obligate dimers with extracellular
domains that recognize small ligands, leading to G-protein activation on the transmembrane …

Structural insights into differences in G protein activation by family A and family B GPCRs

D Hilger, KK Kumar, H Hu, MF Pedersen, ES O'Brien… - Science, 2020 - science.org
INTRODUCTION Transmembrane signaling of heterotrimeric guanine nucleotide–binding
protein (G protein)–coupled receptors (GPCRs) is mediated by ligand-dependent …

Structures of Gi-bound metabotropic glutamate receptors mGlu2 and mGlu4

S Lin, S Han, X Cai, Q Tan, K Zhou, D Wang, X Wang… - Nature, 2021 - nature.com
The metabotropic glutamate receptors (mGlus) have key roles in modulating cell excitability
and synaptic transmission in response to glutamate (the main excitatory neurotransmitter in …

Structure of a D2 dopamine receptor–G-protein complex in a lipid membrane

J Yin, KYM Chen, MJ Clark, M Hijazi, P Kumari, X Bai… - Nature, 2020 - nature.com
The D2 dopamine receptor (DRD2) is a therapeutic target for Parkinson's disease and
antipsychotic drugs. DRD2 is activated by the endogenous neurotransmitter dopamine and …

The pocketome of G-protein-coupled receptors reveals previously untargeted allosteric sites

JB Hedderich, M Persechino, K Becker… - Nature …, 2022 - nature.com
G-protein-coupled receptors do not only feature the orthosteric pockets, where most
endogenous agonists bind, but also a multitude of other allosteric pockets that have come …

Structures of human mGlu2 and mGlu7 homo-and heterodimers

J Du, D Wang, H Fan, C Xu, L Tai, S Lin, S Han, Q Tan… - Nature, 2021 - nature.com
The metabotropic glutamate receptors (mGlus) are involved in the modulation of synaptic
transmission and neuronal excitability in the central nervous system. These receptors …

Mechanisms of adhesion G protein–coupled receptor activation

A Vizurraga, R Adhikari, J Yeung, M Yu… - Journal of Biological …, 2020 - ASBMB
Adhesion G protein–coupled receptors (AGPCRs) are a thirty-three-member subfamily of
Class B GPCRs that control a wide array of physiological processes and are implicated in …

Noncanonical metabotropic glutamate receptor 5 signaling in Alzheimer's disease

KS Abd-Elrahman, SSG Ferguson - Annual Review of …, 2022 - annualreviews.org
Metabotropic glutamate receptor 5 (mGluR5) is ubiquitously expressed in brain regions
responsible for memory and learning. It plays a key role in modulating rapid changes in …