Results 111 to 120 of about 11,641 (225)

Ezrin, Radixin, and Moesin Phosphorylation in NIH3T3 Cells Revealed Angiotensin II Type 1 Receptor Cell-Type–Dependent Biased Signaling

open access: yesJournal of Pharmacological Sciences, 2013
.: β-Arrestin-biased agonists are a new class of drugs with promising therapeutic effects. The molecular mechanisms of β-arrestin-biased agonists are still not completely identified.
Islam A.A.E-H. Ibrahim   +2 more
doaj   +1 more source

Agonist Effects of Propranolol on Non-Tumor Human Breast Cells

open access: yesCells, 2020
The β-blocker propranolol (PROP) has been proposed as a repurposed treatment for breast cancer. The similarity of action between β-agonists and antagonists found on breast cells encouraged us to compare PROP and isoproterenol (ISO, agonist) signaling ...
Lucía Gargiulo   +7 more
doaj   +1 more source

Coping strategies in captive capuchin monkeys (Sapajus spp.) [PDF]

open access: yes, 2016
Studies on diverse species indicate the existence of individual differences in stress coping strategies labelled as ‘proactive’ and ‘reactive’. Identifying taxonomic distribution of such coping strategies is fundamental to evolutionary models and to ...
Aruajo, Talita   +5 more
core   +2 more sources

Biased agonism in peptide-GPCRs: A structural perspective

open access: yesPharmacology & Therapeutics
G protein-coupled receptors (GPCRs) are dynamic membrane receptors that transduce extracellular signals to the cell interior by forming a ligand-receptor-effector (ternary) complex that functions via allosterism. Peptides constitute an important class of ligands that interact with their cognate GPCRs (peptide-GPCRs) to form the ternary complex. "Biased
Tharindunee, Jayakody   +6 more
openaire   +2 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

Conformational Sensors and Domain Swapping Reveal Structural and Functional Differences between β-Arrestin Isoforms

open access: yesCell Reports, 2019
Summary: Desensitization, signaling, and trafficking of G-protein-coupled receptors (GPCRs) are critically regulated by multifunctional adaptor proteins, β-arrestins (βarrs).
Eshan Ghosh   +18 more
doaj   +1 more source

Are we hallucinating or can psychedelic drugs modulate the immune system to control inflammation?

open access: yesBritish Journal of Pharmacology, EarlyView.
Psychedelic drugs that activate 5‐HT2A receptors have been long used for cultural, medicinal and recreational purposes. Interest in psychedelics for treating psychiatric disorders has resurged recently and is well documented; less well recognised are their anti‐inflammatory properties. Growing evidence now demonstrates that psychedelics modulate immune
Omar Qureshi   +10 more
wiley   +1 more source

Psychedelics as pharmacotherapeutics for substance use disorders: A scoping review on clinical trials and perspectives on underlying neurobiology

open access: yesBritish Journal of Pharmacology, EarlyView.
Theorized mechanism of dopamine homeostasis restoration in the nucleus accumbens core induced by a psychedelic intervention. Abstract Psychedelics have garnered great attention in recent years as treatments for major depressive disorder (MDD) and treatment‐resistant depression because of their ability to alter consciousness and afflicted cognitive ...
Lucas Wittenkeller   +3 more
wiley   +1 more source

Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling

open access: yesNature Communications, 2017
Angiotensin II type 1 receptor (AT1R)-mediated acute catecholamine release is modulated by β-arrestin. Here the authors show that β-arrestin-1 recruits the Ca2+channel TRPC3 and the PLCγ to the AT1R-β-arrestin complex, triggering G protein-independent ...
Chun-Hua Liu   +26 more
doaj   +1 more source

G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]

open access: yes, 2017
It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
core   +1 more source

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