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Biased receptor signaling in drug discovery
T Kenakin - Pharmacological reviews, 2019 - Elsevier
A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …
active states that go on to interact with cellular signaling proteins to form a range of different …
Organ‐protective effects and the underlying mechanism of dexmedetomidine
N Bao, B Tang - Mediators of inflammation, 2020 - Wiley Online Library
Dexmedetomidine (DEX) is a highly selective α2 adrenergic receptor (α2AR) agonist
currently used in clinical settings. Because DEX has dose‐dependent advantages of …
currently used in clinical settings. Because DEX has dose‐dependent advantages of …
Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor
Because nonopioid analgesics are much sought after, we computationally docked more
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …
Teaching old receptors new tricks: biasing seven-transmembrane receptors
Abstract Seven-transmembrane receptors (7TMRs; also known as G protein-coupled
receptors) are the largest class of receptors in the human genome and are common targets …
receptors) are the largest class of receptors in the human genome and are common targets …
Biased signaling of G protein coupled receptors (GPCRs): Molecular determinants of GPCR/transducer selectivity and therapeutic potential
G protein coupled receptors (GPCRs) convey signals across membranes via interaction with
G proteins. Originally, an individual GPCR was thought to signal through one G protein …
G proteins. Originally, an individual GPCR was thought to signal through one G protein …
Concurrent stimulation of cannabinoid CB1 and dopamine D2 receptors augments cAMP accumulation in striatal neurons: evidence for a Gs linkage to the CB1 …
Cannabinoids act at the CB1 receptor to inhibit adenylate cyclase activity via a pertussis
toxin-sensitive G-protein. Within the striatum, CB1 receptors have been shown to be …
toxin-sensitive G-protein. Within the striatum, CB1 receptors have been shown to be …
The hippocampus and TNF: Common links between chronic pain and depression
Major depression and chronic pain are significant health problems that seriously impact the
quality of life of affected individuals. These diseases that individually are difficult to treat …
quality of life of affected individuals. These diseases that individually are difficult to treat …
The cannabinoid agonist WIN55,212-2 increases intracellular calcium via CB1 receptor coupling to Gq/11 G proteins
Central nervous system responses to cannabis are primarily mediated by CB1 receptors,
which couple preferentially to Gi/o G proteins. Here, we used calcium photometry to monitor …
which couple preferentially to Gi/o G proteins. Here, we used calcium photometry to monitor …
Molecular basis of receptor/G-protein-coupling selectivity
J Wess - Pharmacology & therapeutics, 1998 - Elsevier
Molecular cloning studies have shown that G-protein-coupled receptors form one of the
largest protein families found in nature, and it is estimated that approximately 1000 different …
largest protein families found in nature, and it is estimated that approximately 1000 different …
Norepinephrine modulates the motility of resting and activated microglia via different adrenergic receptors
S Gyoneva, SF Traynelis - Journal of Biological Chemistry, 2013 - jbc.org
Microglia, the resident immune cells of the central nervous system (CNS), monitor the brain
for disturbances of tissue homeostasis by constantly moving their fine processes. Microglia …
for disturbances of tissue homeostasis by constantly moving their fine processes. Microglia …