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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 …
an important class of drug targets, play a role in maintaining numerous physiological …
G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders
Neuropsychiatric disorders are multifactorial disorders with diverse aetiological factors.
Identifying treatment targets is challenging because the diseases are resulting from …
Identifying treatment targets is challenging because the diseases are resulting from …
Structural basis of odorant recognition by a human odorant receptor
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 …
molecules. This task is accomplished by the combinatorial activation of approximately 400 …
Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT2A
receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5 …
receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5 …
Computational design of soluble and functional membrane protein analogues
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 …
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 …
endogenous agonists bind, but also a multitude of other allosteric pockets that have come …
Sensitive multicolor indicators for monitoring norepinephrine in vivo
Genetically encoded indicators engineered from G-protein-coupled receptors are important
tools that enable high-resolution in vivo neuromodulator imaging. Here, we introduce a …
tools that enable high-resolution in vivo neuromodulator imaging. Here, we introduce a …
Autoregulation of GPCR signalling through the third intracellular loop
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 …
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …
Ligand and G-protein selectivity in the κ-opioid receptor
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 …
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
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 …
by coupling to heterotrimeric G proteins of four classes: G i/o, G q, G s, and G 12/13 …