Involvement of Intramolecular Interactions in the Regulation of G Protein-Coupled Receptor Kinase 2
Molecular Pharmacology, 2003 The G protein-coupled receptor (GPCR) kinase GRK2 phosphorylates G protein-coupled receptors in an agonist-dependent manner. GRK2 activity is modulated through interactions of diverse domains of the kinase with G protein betagamma subunits, several lipids, anchoring proteins, and activated receptors.
Susana, Sarnago +5 more
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G-Protein–Coupled Receptor Kinase Activity in Hypertension [PDF]
Hypertension, 2000 Abstract —Impaired receptor-stimulated adenylyl cyclase activation has been observed in lymphocytes from hypertensive subjects and has been linked to an increase in lymphocyte G-protein receptor kinase-2 (GRK-2) protein expression.
R, Gros +5 more
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Structure of Human G Protein-Coupled Receptor Kinase 2 in Complex with the Kinase Inhibitor Balanol [PDF]
Journal of Medicinal Chemistry, 2010 G protein-coupled receptor kinase 2 (GRK2) is a pharmaceutical target for the treatment of cardiovascular diseases such as congestive heart failure, myocardial infarction, and hypertension. To better understand how nanomolar inhibition and selectivity for GRK2 might be achieved, we have determined crystal structures of human GRK2 in complex with ...
John J G, Tesmer +4 more
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PLoS ONE, 2015 Phosphorylation is a primary modulator of mammalian G-protein coupled receptor (GPCR) activity. The GPCR melanopsin is the photopigment of intrinsically photosensitive retinal ganglion cells (ipRGCs) in the mammalian retina. Recent evidence from in vitro
Timothy J Sexton, Russell N Van Gelder
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Acetate alters the process of lipid metabolism in rabbits
Animal, 2018 An experiment was conducted to investigate the effect of acetate treatment on lipid metabolism in rabbits. New Zealand Rabbits (30 days, n=80) randomly received a subcutaneous injection (2 ml/injection) of 0, 0.5, 1.0 or 2.0 g/kg per day body mass ...
C. Fu, L. Liu, F. Li
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Threonine 180 Is Required for G-protein-coupled Receptor Kinase 3- and β-Arrestin 2-mediated Desensitization of the µ-Opioid Receptor in Xenopus Oocytes [PDF]
, 2001 To determine the sites in the µ-opioid receptor (MOR) critical for agonist-dependent desensitization, we constructed and coexpressed MORs lacking potential phosphorylation sites along with G-protein activated inwardly rectifying potassium channels ...
Celvert, Jeremy P. +4 more
core
The calcium-sensing receptor as a regulator of cellular fate in normal and pathological conditions [PDF]
, 2013 The calcium-sensing receptor (CaSR) belongs to the evolutionarily conserved family of plasma membrane G protein-coupled receptors (GPCRs). Early studies identified an essential role for the CaSR in systemic calcium homeostasis through its ability to ...
Benoit, Yves +3 more
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Sphingosine-1-phosphate signaling and the gut-liver axis in liver diseases
Liver Research, 2019 The liver is the central organ involved in lipid metabolism and the gastrointestinal (GI) tract is responsible for nutrient absorption and partitioning. Obesity, dyslipidemia and metabolic disorders are of increasing public health concern worldwide, and ...
Eric K. Kwong, Huiping Zhou
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The Basal Thermal Sensitivity of the TRPV1 Ion Channel Is Determined by PKCβII [PDF]
, 2014 Copyright © 2014 the authors 0270-6474/14/348246-13$15.00/0.Peer reviewedPublisher ...
Hasan, Raquibul, Li, Lin, Zhang, Xuming
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The G Protein-coupled Receptor Kinase 2 Is a Microtubule-associated Protein Kinase That Phosphorylates Tubulin [PDF]
Journal of Biological Chemistry, 1998 The G protein-coupled receptor kinase 2 (GRK2) is a serine/threonine kinase that phosphorylates and desensitizes agonist-occupied G protein-coupled receptors (GPCRs). Here we demonstrate that GRK2 is a microtubule-associated protein and identify tubulin as a novel GRK2 substrate.
J A, Pitcher +9 more
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