INT81345

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Context Info
Confidence 0.70
First Reported 1999
Last Reported 2007
Negated 1
Speculated 0
Reported most in Abstract
Documents 21
Total Number 21
Disease Relevance 2.89
Pain Relevance 7.90

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
melanocytes 2
EPI 2
embryonic kidney 2
SH-SY5Y 1
plasma 1
ADRBK1 (Homo sapiens)
ADRBK1 - K220R (1)
Pain Link Frequency Relevance Heat
melanocortin 1 receptor 28 99.18 Very High Very High Very High
agonist 229 98.52 Very High Very High Very High
Morphine 14 97.84 Very High Very High Very High
Catecholamine 45 97.64 Very High Very High Very High
Kinase C 34 95.68 Very High Very High Very High
Enkephalin 2 94.64 High High
Inflammation 12 94.56 High High
mu opioid receptor 5 93.08 High High
tolerance 8 91.52 High High
potassium channel 3 91.36 High High
Disease Link Frequency Relevance Heat
Skin Cancer 19 100.00 Very High Very High Very High
INFLAMMATION 12 94.56 High High
Bordatella Infection 5 92.32 High High
Neuroblastoma 52 89.48 High High
Asthma 43 86.44 High High
Hyperalgesia 2 70.56 Quite High
Dysmenorrhea 2 64.76 Quite High
Occupational Lung Diseases 9 60.96 Quite High
Viral Infection 1 51.96 Quite High
Disease 14 6.00 Low Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
In COS-7 cells, which express low levels of GRK2 and beta-arrestin, overexpression of GRK2 and beta-arrestin increased receptor phosphorylation, desensitization, and internalization to the high levels observed in human embryonic kidney 293 cells.
Gene_expression (overexpression) of GRK2 in embryonic kidney
1) Confidence 0.70 Published 2004 Journal Mol. Endocrinol. Section Abstract Doc Link 14976224 Disease Relevance 0.06 Pain Relevance 0.13
In COS-7 cells, which express low levels of GRK2 and beta-arrestin, overexpression of GRK2 and beta-arrestin increased receptor phosphorylation, desensitization, and internalization to the high levels observed in human embryonic kidney 293 cells.
Gene_expression (express) of GRK2 in embryonic kidney
2) Confidence 0.70 Published 2004 Journal Mol. Endocrinol. Section Abstract Doc Link 14976224 Disease Relevance 0.06 Pain Relevance 0.14
Both melanoma cells and normal melanocytes express two members of the G protein-coupled receptor kinase (GRK) family, GRK2 and GRK6.
Gene_expression (express) of GRK2 in melanocytes associated with skin cancer
3) Confidence 0.66 Published 2005 Journal Mol. Endocrinol. Section Abstract Doc Link 15650023 Disease Relevance 0.41 Pain Relevance 0.73
Cotransfection of the receptor and GRK2 or GRK6 genes in heterologous cells demonstrated that GRK2 and GRK6 impair agonist-dependent signaling by MC1R or Mc1r.
Gene_expression (Cotransfection) of GRK2 associated with melanocortin 1 receptor and agonist
4) Confidence 0.66 Published 2005 Journal Mol. Endocrinol. Section Abstract Doc Link 15650023 Disease Relevance 0.41 Pain Relevance 0.74
Expression of a dominant negative GRK2 mutant in melanoma cells increased their cAMP response to agonists.
Gene_expression (Expression) of GRK2 associated with agonist and skin cancer
5) Confidence 0.66 Published 2005 Journal Mol. Endocrinol. Section Abstract Doc Link 15650023 Disease Relevance 0.42 Pain Relevance 0.76
Comparing the effect of over-expressed GRK2 and GRK3 on sequestration of kappa-receptors, we conclude that GRK3 more strongly induces kappa-receptor internalization than GRK2.
Gene_expression (expressed) of GRK2
6) Confidence 0.63 Published 2002 Journal Mol. Pharmacol. Section Abstract Doc Link 12021406 Disease Relevance 0 Pain Relevance 0.15
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.
Gene_expression (levels) of GRK2 in C cells
7) Confidence 0.62 Published 2002 Journal Neuropharmacology Section Abstract Doc Link 12423667 Disease Relevance 0.09 Pain Relevance 0.30
Antisense DNA treatment confirmed the involvement of GRK2/3 in mu and ORL1 desensitization.
Gene_expression (desensitization) of GRK2
8) Confidence 0.62 Published 2002 Journal Neuropharmacology Section Abstract Doc Link 12423667 Disease Relevance 0.06 Pain Relevance 0.52
We have shown that MC1R desensitization is mediated by two GRKs expressed in melanocytes and melanoma cells, GRK2 and GRK6.
Gene_expression (expressed) of GRK2 in melanocytes associated with melanocortin 1 receptor and skin cancer
9) Confidence 0.55 Published 2007 Journal J. Biol. Chem. Section Abstract Doc Link 17130136 Disease Relevance 0.31 Pain Relevance 0.67
However, DAMGO (1 microM) pretreatment increased membrane levels of GRK2 and GRK3, indicating their translocation to the membrane upon activation.
Gene_expression (levels) of GRK2
10) Confidence 0.49 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12750434 Disease Relevance 0.22 Pain Relevance 0.77
Expression of a dominant negative mutant G protein-coupled receptor kinase 2 (GRK2), GRK2-K220R, markedly attenuated the DAMGO-induced desensitization of MOR1, but it had no effect on morphine-induced MOR1 desensitization.
Gene_expression (Expression) of GRK2 associated with morphine
11) Confidence 0.45 Published 2006 Journal Mol. Pharmacol. Section Abstract Doc Link 16682505 Disease Relevance 0 Pain Relevance 1.46
While co-expression of the wild type GRK2, beta-arrestin, or dynamin I had no effect on kappa receptor internalization, co-expression of the dominant negative mutants GRK2-K220R, beta-arrestin (319-418), or dynamin I-K44A significantly inhibited receptor internalization.
Gene_expression (co-expression) of GRK2
12) Confidence 0.37 Published 1999 Journal J. Biol. Chem. Section Abstract Doc Link 10207034 Disease Relevance 0.09 Pain Relevance 0.45
While co-expression of the wild type GRK2, beta-arrestin, or dynamin I had no effect on kappa receptor internalization, co-expression of the dominant negative mutants GRK2-K220R, beta-arrestin (319-418), or dynamin I-K44A significantly inhibited receptor internalization.
Gene_expression (co-expression) of GRK2 (K220R)
13) Confidence 0.37 Published 1999 Journal J. Biol. Chem. Section Abstract Doc Link 10207034 Disease Relevance 0.09 Pain Relevance 0.47
adrenergic receptor kinase (GRK2 and 3); and GRK4 group (GRK4, 5 and 6).
Gene_expression (group) of GRK2
14) Confidence 0.37 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2644495 Disease Relevance 0 Pain Relevance 0.11
GRK2 and GRK3 require the ??
Gene_expression (require) of GRK2
15) Confidence 0.33 Published 2007 Journal BMC Pharmacol Section Body Doc Link PMC2234403 Disease Relevance 0 Pain Relevance 0
Chronic EPI exposure does not alter GRK2 or GRK3 levels in whole cells but instead enhances GRK2 and GRK3 expression at the membrane in SH?
Gene_expression (levels) of GRK2 in EPI
16) Confidence 0.33 Published 2007 Journal BMC Pharmacol Section Body Doc Link PMC2234403 Disease Relevance 0 Pain Relevance 0.07
Chronic EPI exposure altered neither GRK3 nor GRK2 levels in the transfected SH-SY5Y cell line (Table 4).
Neg (neither) Gene_expression (levels) of GRK2 in SH-SY5Y
17) Confidence 0.33 Published 2007 Journal BMC Pharmacol Section Body Doc Link PMC2234403 Disease Relevance 0 Pain Relevance 0.05
Chronic EPI exposure does not alter GRK2 or GRK3 levels in whole cells but instead enhances GRK2 and GRK3 expression at the membrane in SH?
Gene_expression (expression) of GRK2 in EPI
18) Confidence 0.33 Published 2007 Journal BMC Pharmacol Section Body Doc Link PMC2234403 Disease Relevance 0 Pain Relevance 0.07
2A-AR prompts enhanced expression of GRK3, but not GRK2, in whole cells [15] and membrane fractions.
Gene_expression (expression) of GRK2
19) Confidence 0.29 Published 2007 Journal BMC Pharmacol Section Body Doc Link PMC2234403 Disease Relevance 0 Pain Relevance 0
2-ARs does not increase either GRK3 or GRK2 expression per se, but does increase translocation of GRK2 and GRK3 to the plasma membrane.
Gene_expression (expression) of GRK2 in plasma
20) Confidence 0.29 Published 2007 Journal BMC Pharmacol Section Body Doc Link PMC2234403 Disease Relevance 0 Pain Relevance 0

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