Review of the endocannabinoid system
The endocannabinoid system (ECS) is a widespread neuromodulatory network involved in
the developing central nervous system as well as playing a major role in tuning many …
the developing central nervous system as well as playing a major role in tuning many …
Psychedelics in psychiatry: neuroplastic, immunomodulatory, and neurotransmitter mechanisms
Mounting evidence suggests safety and efficacy of psychedelic compounds as potential
novel therapeutics in psychiatry. Ketamine has been approved by the Food and Drug …
novel therapeutics in psychiatry. Ketamine has been approved by the Food and Drug …
GPCR activation mechanisms across classes and macro/microscales
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome
G-protein-coupled receptors (GPCRs) remain major drug targets, despite our incomplete
understanding of how they signal through 16 non-visual G-protein signal transducers …
understanding of how they signal through 16 non-visual G-protein signal transducers …
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 …
Virtual discovery of melatonin receptor ligands to modulate circadian rhythms
RM Stein, HJ Kang, JD McCorvy, GC Glatfelter… - Nature, 2020 - nature.com
The neuromodulator melatonin synchronizes circadian rhythms and related physiological
functions through the actions of two G-protein-coupled receptors: MT1 and MT2. Circadian …
functions through the actions of two G-protein-coupled receptors: MT1 and MT2. Circadian …
GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation
G protein-coupled receptors (GPCRs) activate G proteins and undergo a complex regulation
by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes …
by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes …
Molecular basis of β-arrestin coupling to formoterol-bound β1-adrenoceptor
Y Lee, T Warne, R Nehmé, S Pandey… - Nature, 2020 - nature.com
Abstract The β1-adrenoceptor (β1AR) is a G-protein-coupled receptor (GPCR) that couples
to the heterotrimeric G protein Gs. G-protein-mediated signalling is terminated by …
to the heterotrimeric G protein Gs. G-protein-mediated signalling is terminated by …
Common coupling map advances GPCR-G protein selectivity
Two-thirds of human hormones and one-third of clinical drugs act on membrane receptors
that couple to G proteins to achieve appropriate functional responses. While G protein …
that couple to G proteins to achieve appropriate functional responses. While G protein …
Combinatorial expression of GPCR isoforms affects signalling and drug responses
M Marti-Solano, SE Crilly, D Malinverni, C Munk… - Nature, 2020 - nature.com
G-protein-coupled receptors (GPCRs) are membrane proteins that modulate physiology
across human tissues in response to extracellular signals. GPCR-mediated signalling can …
across human tissues in response to extracellular signals. GPCR-mediated signalling can …