Results 81 to 90 of about 45,700 (234)

Light-Dependent Translocation of Arrestin in the Absence of Rhodopsin Phosphorylation and Transducin Signaling [PDF]

open access: yes, 2003
Visual arrestin plays a crucial role in the termination of the light response in vertebrate photoreceptors by binding selectively to light-activated, phosphorylated rhodopsin.
Chen, Jeannie   +3 more
core  

The α-Arrestin ARRDC3 Regulates the Endosomal Residence Time and Intracellular Signaling of the β2-Adrenergic Receptor. [PDF]

open access: yes, 2016
Arrestin domain-containing protein 3 (ARRDC3) is a member of the mammalian α-arrestin family, which is predicted to share similar tertiary structure with visual-/β-arrestins and also contains C-terminal PPXY motifs that mediate interaction with E3 ...
Benovic, Jeffrey L.   +6 more
core   +2 more sources

Preclinical models for evaluating psychedelics in the treatment of major depressive disorder

open access: yesBritish Journal of Pharmacology, EarlyView.
Psychedelic drugs have seen a resurgence in interest as a next generation of psychiatric medicines with potential as rapid‐acting antidepressants (RAADs). Despite promising early clinical trials, the mechanisms which underlie the effects of psychedelics are poorly understood.
Laith Alexander   +5 more
wiley   +1 more source

Signaling bias of the protease-activated receptor-1 is dictated by distinct GRK5 and β-arrestin-2 determinants

open access: yesCell Reports
Summary: G protein-coupled receptors (GPCRs) exhibit signaling bias or preferential activation of heterotrimeric G proteins versus GPCR kinase (GRK)-mediated β-arrestin signaling.
Monica L. Gonzalez Ramirez   +7 more
doaj   +1 more source

Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]

open access: yes, 2018
The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E   +4 more
core  

Pepducins as a potential treatment strategy for asthma and COPD. [PDF]

open access: yes, 2018
Current therapies to treat asthma and other airway diseases primarily include anti-inflammatory agents and bronchodilators. Anti-inflammatory agents target trafficking and resident immunocytes and structural cells, while bronchodilators act to prevent or
Benovic, Jeffrey L.   +4 more
core   +2 more sources

Neuropsychopharmacology of hallucinogenic and non‐hallucinogenic 5‐HT2A receptor agonists

open access: yesBritish Journal of Pharmacology, EarlyView.
Psychedelic drugs such as LSD and psilocin were once relegated to the fringes of medical research because of their association with counterculture movements and a perceived concern about harm through recreational use, and their consequent legal prohibition in the early 1970s.
Trevor Sharp, Aurelija Ippolito
wiley   +1 more source

Quinolones modulate ghrelin receptor signaling: potential for a novel small molecule scaffold in the treatment of cachexia [PDF]

open access: yes, 2018
Cachexia is a metabolic wasting disorder characterized by progressive weight loss, muscle atrophy, fatigue, weakness, and appetite loss. Cachexia is associated with almost all major chronic illnesses including cancer, heart failure, obstructive ...
Cano, Rafael   +8 more
core   +3 more sources

Evidence that 5‐HT2A receptor signalling efficacy and not biased agonism differentiates serotonergic psychedelic from non‐psychedelic drugs

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Serotonergic psychedelic drugs are under investigation as therapies for various psychiatric disorders, including major depression. Although serotonergic psychedelic drugs are 5‐HT2A receptor agonists, some such agonists are not psychedelic, potentially due to differences in 5‐HT2A receptor ligand bias or signalling efficacy. Here,
Aurelija Ippolito   +6 more
wiley   +1 more source

Emerging Roles of β-Arrestins [PDF]

open access: yesCell Cycle, 2006
Arrestins were originally characterized as structural adaptor proteins which modulate the desensitization and trafficking of seven-membrane-spanning receptors. From these seminal observations a multitude of novel functions for this gene family have arisen. Here we review the recently identified roles for beta-arrestin including its nuclear function and
F Gregory, Buchanan, Raymond N, DuBois
openaire   +2 more sources

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