GPR54 regulates ERK1/2 activity and hypothalamic gene expression in a Gα(q/11) and β-arrestin-dependent manner. [PDF]
PLoS ONE, 2010 G protein-coupled receptor 54 (GPR54) is a G(q/11)-coupled 7 transmembrane-spanning receptor (7TMR). Activation of GPR54 by kisspeptin (Kp) stimulates PIP(2) hydrolysis, Ca(2+) mobilization and ERK1/2 MAPK phosphorylation.
Jacob M Szereszewski +5 more
doaj +1 more source
Pulmonary Circulation, 2022 Modulation of endothelial cell behavior and phenotype by hemodynamic forces involves many signaling components, including cell surface receptors, intracellular signaling intermediaries, transcription factors, and epigenetic elements.
Saejeong Park +9 more
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
The endocytosis of oxidized LDL via the activation of the angiotensin II type 1 receptor
iScience, 2021 Summary: Arrestin-dependent activation of a G-protein-coupled receptor (GPCR) triggers endocytotic internalization of the receptor complex. We analyzed the interaction between the pattern recognition receptor (PRR) lectin-like oxidized low-density ...
Toshimasa Takahashi +23 more
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Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s) [PDF]
, 2015 ACKNOWLEDGMENTS The work was supported by National Institutes of Health grants DA027113 and EY024717 to G.A.T. and DA09158 to A.M. A portion of this work was submitted in 2011 by A. Kulkarni in partial fulfillment of M.S.
Cascio, Maria G. +12 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
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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
β-Arrestin-Mediated Signaling Improves the Efficacy of Therapeutics
Journal of Pharmacological Sciences, 2012 β-Arrestins (β-arrestin-1 and β-arrestin-2) were first identified as proteins that have the ability to desensitize G protein-coupled receptors (GPCRs). However, it has recently been found that β-arrestins can activate signaling pathways independent of G ...
Islam A.A.E.-H. Ibrahim, Hitoshi Kurose
doaj +1 more source
B-arrestin-2 Signaling Is Important to Preserve Cardiac Function During Aging
Frontiers in Physiology, 2021 Experiments reported here tested the hypothesis that β-arrestin-2 is an important element in the preservation of cardiac function during aging. We tested this hypothesis by aging β-arrestin-2 knock-out (KO) mice, and wild-type equivalent (WT) to 12 ...
Andrielle E. Capote +7 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