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 …

G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders

TS Wong, G Li, S Li, W Gao, G Chen, S Gan… - … and Targeted Therapy, 2023 - nature.com
Neuropsychiatric disorders are multifactorial disorders with diverse aetiological factors.
Identifying treatment targets is challenging because the diseases are resulting from …

Structural basis of odorant recognition by a human odorant receptor

CB Billesbølle, CA de March, WJC van der Velden… - Nature, 2023 - nature.com
Our sense of smell enables us to navigate a vast space of chemically diverse odour
molecules. This task is accomplished by the combinatorial activation of approximately 400 …

Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential

J Wallach, AB Cao, MM Calkins, AJ Heim… - Nature …, 2023 - nature.com
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT2A
receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5 …

Computational design of soluble and functional membrane protein analogues

CA Goverde, M Pacesa, N Goldbach, LJ Dornfeld… - Nature, 2024 - nature.com
De novo design of complex protein folds using solely computational means remains a
substantial challenge. Here we use a robust deep learning pipeline to design complex folds …

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 …

Sensitive multicolor indicators for monitoring norepinephrine in vivo

Z Kagiampaki, V Rohner, C Kiss, S Curreli, A Dieter… - Nature …, 2023 - nature.com
Genetically encoded indicators engineered from G-protein-coupled receptors are important
tools that enable high-resolution in vivo neuromodulator imaging. Here, we introduce a …

Autoregulation of GPCR signalling through the third intracellular loop

F Sadler, N Ma, M Ritt, Y Sharma, N Vaidehi… - Nature, 2023 - nature.com
The third intracellular loop (ICL3) of the G protein-coupled receptor (GPCR) fold is important
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …

Ligand and G-protein selectivity in the κ-opioid receptor

J Han, J Zhang, AL Nazarova, SM Bernhard… - Nature, 2023 - nature.com
The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not
only pain but also addiction and affective disorders. However, the development of KOR …

[HTML][HTML] Rules and mechanisms governing G protein coupling selectivity of GPCRs

I Masuho, R Kise, P Gainza, E Von Moo, X Li, R Tany… - Cell reports, 2023 - cell.com
G protein-coupled receptors (GPCRs) convert extracellular stimuli into intracellular signaling
by coupling to heterotrimeric G proteins of four classes: G i/o, G q, G s, and G 12/13 …