β-Arrestin-dependent deactivation of mouse melanopsin.
PLoS ONE, 2014 In mammals, the expression of the unusual visual pigment, melanopsin, is restricted to a small subset of intrinsically photosensitive retinal ganglion cells (ipRGCs), whose signaling regulate numerous non-visual functions including sleep, circadian ...
Evan G Cameron, Phyllis R Robinson
doaj +1 more source
Unraveling the molecular architecture of a G protein-coupled receptor/β-arrestin/Erk module complex [PDF]
, 2015 International audienceβ-arrestins serve as signaling scaffolds downstream of G protein-coupled receptors, and thus play a crucial role in a plethora of cellular processes.
Azé, Jérôme +6 more
core +4 more sources
β-Arrestin regulation of myosin light chain phosphorylation promotes AT1aR-mediated cell contraction and migration. [PDF]
PLoS ONE, 2013 Over the last decade, it has been established that G-protein-coupled receptors (GPCRs) signal not only through canonical G-protein-mediated mechanisms, but also through the ubiquitous cellular scaffolds β-arrestin-1 and β-arrestin-2.
Elie Simard +5 more
doaj +1 more source
Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators [PDF]
, 2016 This Letter was supported by the Biotechnology and Biological Sciences Research Council (BBSRC) and the Scottish Universities Life Sciences Alliance (SULSA) in 2011Peer ...
Abdelrahman, Mostafa Hamed +4 more
core +1 more source
G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]
, 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
Beta-Arrestins in the Treatment of Heart Failure Related to Hypertension: A Comprehensive Review
Pharmaceutics, 2021 Heart failure (HF) is a complicated clinical syndrome that is considered an increasingly frequent reason for hospitalization, characterized by a complex therapeutic regimen, reduced quality of life, and high morbidity.
Ahmed Rakib +10 more
doaj +1 more source
Differential Signaling Profiles of MC4R Mutations with Three Different Ligands [PDF]
, 2020 The melanocortin 4 receptor (MC4R) is a key player in hypothalamic weight regulation and energy expenditure as part of the leptin-melanocortin pathway. Mutations in this G protein coupled receptor (GPCR) are the most common cause for monogenetic obesity,
Annibale, Paolo +8 more
core +3 more sources
Frontiers in Pharmacology, 2013 A limited number of biomarkers in the central and peripheral systems which are known may be useful for diagnosing major depressive disorders and predicting the effectiveness of antidepressant treatments.
Indira eMENDEZ-DAVID +7 more
doaj +1 more source
Surfactant protein-A modulates LPS-induced TLR4 localization and signaling via β-arrestin 2. [PDF]
PLoS ONE, 2013 The soluble C-type lectin surfactant protein (SP)-A mediates lung immune responses partially via its direct effects on alveolar macrophages (AM), the main resident leukocytes exposed to antigens. SP-A modulates the AM threshold of lipopolysaccharide (LPS)
Vicky Sender, Linda Lang, Cordula Stamme
doaj +1 more source
Long receptor residence time of C26 contributes to super agonist activity at the human β2 adrenoceptor [PDF]
, 2016 Super agonists produce greater functional responses than endogenous agonists in the same assay, and their unique pharmacology is the subject of increasing interest and debate. We propose that receptor residence time and the duration of receptor signaling
Bradley, Michelle E. +9 more
core +1 more source