ATHENA: A Phase 3, Open-Label Study Of The Safety And Effectiveness Of Oliceridine (TRV130), A G-Protein Selective Agonist At The µ-Opioid Receptor, In Patients With Moderate To Severe Acute Pain Requiring Parenteral Opioid Therapy. [PDF]
, 2019 Background:Pain management with conventional opioids can be challenging due to dose-limiting adverse events (AEs), some of which may be related to the simultaneous activation of β-arrestin (a signaling pathway associated with opioid-related AEs) and G ...
Beard, Timothy L +10 more
core
Differential β-arrestin2 requirements for constitutive and agonist-induced internalization of the CB1 cannabinoid receptor [PDF]
, 2013 CB1 cannabinoid receptor (CB1R) undergoes both constitutive and agonist-induced internalization, but the underlying mechanisms of these processes and the role of beta-arrestins in the regulation of CB1R function are not completely understood.
Ahn +64 more
core +1 more source
Diabetes, Obesity and Metabolism, EarlyView.Abstract Aims To assess the glycaemic efficacy and safety of CT‐868, a cAMP signal‐biased, dual glucagon‐like peptide‐1/glucose‐dependent insulinotropic polypeptide receptor agonist, in participants with type 2 diabetes (T2D). Materials and Methods This 26‐week (W), phase 2, randomized, double‐blind placebo‐controlled trial enrolled adults with T2D ...
Manu V. Chakravarthy +10 more
wiley +1 more source
Considering the role of Murine double minute 2 in the cardiovascular system [PDF]
, 2019 The E3 ubiquitin ligase Murine double minute 2 (MDM2) is the main negative regulator of the tumor protein p53 (TP53). Extensive studies over more than two decades have confirmed MDM2 oncogenic role through mechanisms both TP53-dependent and TP53 ...
Lam, Brian, Roudier, Emile
core +1 more source
Lock, relax, load, and shoot: a molecular perspective on Nedd4 regulation
The FEBS Journal, EarlyView.Structural basis of inactive and active states of the Nedd4 HECT E3 ligase subfamily, following a ‘lock, relax, load, and shoot’ mechanism. In the locked, autoinhibited state, intramolecular domain interactions restrain the HECT domain. Relaxation releases these restraints, allowing loading of ubiquitin onto the catalytic cysteine, followed by the ...
Masa Janosev +2 more
wiley +1 more source
Behavioral Characterization of β-Arrestin 1 Knockout Mice in Anxiety-Like and Alcohol Behaviors
Frontiers in Behavioral Neuroscience, 2018 β-Arrestin 1 and 2 are highly expressed proteins involved in the desensitization of G protein-coupled receptor signaling which also regulate a variety of intracellular signaling pathways.
Meridith T. Robins +5 more
doaj +1 more source
Galanin receptor 2 modifies neuropeptide Y Y1 receptor internalization and β-Arrestin recruitment [PDF]
, 2015 We have recently described a Galanin receptor 2(GALR2) and Neuropeptide Y Y1 receptor(NPYY1R) interaction at behavioural, cellular and receptor levels through GALR2/NPYY1R heterodimers.
Borroto-Escuela, Dasiel +8 more
core
Pharmacogenetics of analgesic drugs [PDF]
, 2013 • Individual variability in pain perception and differences in the efficacy of analgesic drugs are complex phenomena and are partly genetically predetermined.
Branford, R +4 more
core +1 more source
Melatonin and the Dental Pulp: A Scoping Review
International Endodontic Journal, EarlyView.ABSTRACT Background In general medicine, melatonin is known to enhance wound healing and promote stem cell differentiation. Its potential relevance in endodontics, however, remains underexplored. Objectives This scoping review aimed to systematically assess the available evidence on the effects of melatonin (a) on dental pulp tissue and (b) on human ...
Jasmin Schäfer +2 more
wiley +1 more source