Allosteric modulation of G protein-coupled receptor signaling

S Shen, C Zhao, C Wu, S Sun, Z Li, W Yan… - Frontiers in …, 2023 - frontiersin.org
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins,
regulate a wide array of physiological processes in response to extracellular signals …

G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery

M Zhang, T Chen, X Lu, X Lan, Z Chen… - Signal Transduction and …, 2024 - nature.com
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

Positive allosteric modulation of a GPCR ternary complex

WAC Burger, CJ Draper-Joyce, C Valant… - Science …, 2024 - science.org
The activation of a G protein–coupled receptor (GPCR) leads to the formation of a ternary
complex between agonist, receptor, and G protein that is characterized by high-affinity …

Concerted conformational changes control metabotropic glutamate receptor activity

N Lecat-Guillet, RB Quast, H Liu, E Bourrier… - Science …, 2023 - science.org
Allosteric modulators bear great potential to fine-tune neurotransmitter action. Promising
targets are metabotropic glutamate (mGlu) receptors, which are associated with numerous …

Cholesterol in Class C GPCRs: Role, relevance, and localization

UH Isu, SA Badiee, E Khodadadi, M Moradi - Membranes, 2023 - mdpi.com
G-protein coupled receptors (GPCRs), one of the largest superfamilies of cell-surface
receptors, are heptahelical integral membrane proteins that play critical roles in virtually …

Conformational coupling between extracellular and transmembrane domains modulates holo-adhesion GPCR function

SP Kordon, K Cechova, SJ Bandekar, K Leon… - Nature …, 2024 - nature.com
Abstract Adhesion G Protein-Coupled Receptors (aGPCRs) are key cell-adhesion
molecules involved in numerous physiological functions. aGPCRs have large multi-domain …

Stepwise activation of a metabotropic glutamate receptor

K Krishna Kumar, H Wang, C Habrian, NR Latorraca… - Nature, 2024 - nature.com
Metabotropic glutamate receptors belong to a family of G protein-coupled receptors that are
obligate dimers and possess a large extracellular ligand-binding domain that is linked via a …

Structural analysis and conformational dynamics of a holo-adhesion GPCR reveal interplay between extracellular and transmembrane domains

SP Kordon, K Cechova, SJ Bandekar, K Leon, P Dutka… - bioRxiv, 2024 - biorxiv.org
ABSTRACT Adhesion G Protein-Coupled Receptors (aGPCRs) are key cell-adhesion
molecules involved in numerous physiological functions. aGPCRs have large multi-domain …

[HTML][HTML] Step-wise activation of a Family C GPCR

KK Kumar, H Wang, C Habrian, NR Latorraca, J Xu… - Biorxiv, 2023 - ncbi.nlm.nih.gov
Metabotropic glutamate receptors belong to a family of G protein-coupled receptors that are
obligate dimers and possess a large extracellular ligand-binding domain (ECD) that is …

Structural basis of allosteric modulation of metabotropic glutamate receptor activation and desensitization

A Strauss, AJ Gonzalez-Hernandez, J Lee, N Abreu… - bioRxiv, 2023 - biorxiv.org
The metabotropic glutamate receptors (mGluRs) are neuromodulatory family CG protein
coupled receptors which assemble as dimers and allosterically couple extracellular ligand …