INT100741

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Context Info
Confidence 0.64
First Reported 2002
Last Reported 2007
Negated 1
Speculated 0
Reported most in Abstract
Documents 10
Total Number 10
Disease Relevance 1.01
Pain Relevance 3.95

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

cytosol (ADRBK1) signal transduction (ADRBK1) aging (ADRBK1)
plasma membrane (ADRBK1) cytoplasm (ADRBK1)
Anatomy Link Frequency
SH-SY5Y 1
EPI 1
C cells 1
ADRBK1 (Homo sapiens)
Pain Link Frequency Relevance Heat
Kinase C 20 100.00 Very High Very High Very High
mu opioid receptor 13 99.76 Very High Very High Very High
agonist 29 99.12 Very High Very High Very High
Enkephalin 4 95.40 Very High Very High Very High
tolerance 15 94.04 High High
opioid receptor 18 93.04 High High
MU agonist 5 92.40 High High
Delta opioid receptors 1 90.00 High High
orphanin 19 83.12 Quite High
Opioid 4 79.24 Quite High
Disease Link Frequency Relevance Heat
Neuroblastoma 19 89.96 High High
Glioma 1 75.96 Quite High
Hyperalgesia 2 71.32 Quite High
Aids-related Complex 3 5.00 Very Low Very Low Very Low
Pain 1 5.00 Very Low Very Low Very Low
Hypertension 1 5.00 Very Low Very Low Very Low
Sleep Disorders 1 5.00 Very Low Very Low Very Low
Cv General 4 Under Development 1 5.00 Very Low Very Low Very Low
Depression 1 5.00 Very Low Very Low Very Low
Leukemia 1 5.00 Very Low Very Low Very Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Upregulation of GRK2 correlated with increases in levels of transcription factors Sp1 or AP-2.
Positive_regulation (Upregulation) of GRK2
1) Confidence 0.64 Published 2002 Journal Neuropharmacology Section Abstract Doc Link 12423667 Disease Relevance 0.08 Pain Relevance 0.31
In contrast to delta-receptors, mu-receptors failed to trigger accumulation of GRK2 or 3 at the membrane, and no cointernalization of mu-opioid receptors with GRK2 or 3 was observed.
Positive_regulation (accumulation) of GRK2 associated with mu opioid receptor
2) Confidence 0.59 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 11805194 Disease Relevance 0.15 Pain Relevance 0.35
However, DAMGO (1 microM) pretreatment increased membrane levels of GRK2 and GRK3, indicating their translocation to the membrane upon activation.
Positive_regulation (increased) of GRK2
3) Confidence 0.57 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12750434 Disease Relevance 0.22 Pain Relevance 0.78
Induction of G protein-coupled receptor kinases 2 and 3 contributes to the cross-talk between mu and ORL1 receptors following prolonged agonist exposure.
Positive_regulation (Induction) of protein-coupled receptor kinases 2 associated with agonist
4) Confidence 0.55 Published 2002 Journal Neuropharmacology Section Title Doc Link 12423667 Disease Relevance 0.09 Pain Relevance 0.31
Prolonged ORL1 activation increased GRK2 levels and desensitized both receptors in SH-SY5Y cells.
Positive_regulation (increased) of GRK2 in SH-SY5Y
5) Confidence 0.46 Published 2002 Journal Neuropharmacology Section Abstract Doc Link 12423667 Disease Relevance 0.09 Pain Relevance 0.31
We also demonstrate that chronic OFQ/N-mediated desensitization of ORL1 and mu receptors occurs via cell-specific pathways, involving ERK1/2-dependent GRK2, or PKC-dependent and ERK1/2-independent GRK3 induction.
Neg (independent) Positive_regulation (induction) of GRK2 associated with kinase c
6) Confidence 0.46 Published 2002 Journal Neuropharmacology Section Abstract Doc Link 12423667 Disease Relevance 0 Pain Relevance 0.42
Prolonged (24 h) activation of the mu receptor desensitized both mu and ORL1 receptor-mediated inhibition of forskolin-stimulated cAMP accumulation and upregulated GRK2 levels in SH-SY5Y and BE(2)-C cells.
Positive_regulation (upregulated) of GRK2 in C cells
7) Confidence 0.43 Published 2002 Journal Neuropharmacology Section Abstract Doc Link 12423667 Disease Relevance 0.09 Pain Relevance 0.30
This suggests that DAMGO activation of mu-opioid receptors results in GRK2 and GRK3 inactivation of ORL1 upon challenge with OFQ/N.
Positive_regulation (inactivation) of GRK2 associated with mu opioid receptor
8) Confidence 0.41 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12750434 Disease Relevance 0.22 Pain Relevance 0.76
These data suggest that OFQ/N binds to NOP receptors and activates protein kinase C, which then increases the ability of GRK2 to phosphorylate the agonist-occupied mu receptor, heterologously regulating homologous mu receptor desensitization.
Positive_regulation (increases) of GRK2 associated with kinase c and agonist
9) Confidence 0.37 Published 2005 Journal Mol. Pharmacol. Section Abstract Doc Link 15890842 Disease Relevance 0.06 Pain Relevance 0.41
Therefore, this increased GRK2 and GRK3 translocation to the membrane following prolonged EPI treatment in SH?
Positive_regulation (increased) of GRK2 in EPI
10) Confidence 0.23 Published 2007 Journal BMC Pharmacol Section Body Doc Link PMC2234403 Disease Relevance 0 Pain Relevance 0

General Comments

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