INT85677

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Context Info
Confidence 0.68
First Reported 1999
Last Reported 2011
Negated 0
Speculated 0
Reported most in Body
Documents 24
Total Number 25
Disease Relevance 8.41
Pain Relevance 4.09

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

signal transduction (Gpbar1) plasma membrane (Gpbar1) signal transducer activity (Gpbar1)
Anatomy Link Frequency
dendritic cells 1
lungs 1
central nervous system 1
T cell 1
Gpbar1 (Mus musculus)
Pain Link Frequency Relevance Heat
antagonist 100 100.00 Very High Very High Very High
agonist 269 99.96 Very High Very High Very High
Pain 50 99.92 Very High Very High Very High
mu opioid receptor 5 99.72 Very High Very High Very High
Morphine 14 99.56 Very High Very High Very High
amygdala 108 99.52 Very High Very High Very High
Inflammation 39 99.52 Very High Very High Very High
alcohol 30 99.12 Very High Very High Very High
Central nervous system 1 99.04 Very High Very High Very High
Serotonin 11 99.00 Very High Very High Very High
Disease Link Frequency Relevance Heat
Pain 53 99.92 Very High Very High Very High
INFLAMMATION 47 99.52 Very High Very High Very High
Apoptosis 118 98.84 Very High Very High Very High
Breast Cancer 14 97.56 Very High Very High Very High
Prostate Cancer 68 97.04 Very High Very High Very High
Metastasis 40 97.00 Very High Very High Very High
Depression 4 96.56 Very High Very High Very High
Death 5 96.08 Very High Very High Very High
Cancer 152 95.88 Very High Very High Very High
Anxiety Disorder 219 94.36 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
GPCR activation is determined not only by the initiation of signaling cascades but also by regulatory mechanisms that control the extent and duration of their signals.
Positive_regulation (activation) of GPCR
1) Confidence 0.68 Published 2004 Journal Neuromolecular Med. Section Abstract Doc Link 15001811 Disease Relevance 0.27 Pain Relevance 0.32
G protein-coupled receptor kinase 5 (GRK5) is a member of a family of enzymes that phosphorylate activated G protein-coupled receptors (GPCR).
Positive_regulation (activated) of GPCR
2) Confidence 0.55 Published 1999 Journal Neuron Section Abstract Doc Link 10624964 Disease Relevance 0.22 Pain Relevance 0.07
Recently, two novel Rho-specific guanine nucleotide exchange factors (RhoGEFs), PDZ-RhoGEF and LARG, have been identified to interact with the activated alpha-subunits of G12/G13 and are thus believed to mediate GPCR-induced Rho activation.
Positive_regulation (activation) of GPCR
3) Confidence 0.45 Published 2002 Journal Eur. J. Neurosci. Section Abstract Doc Link 12492428 Disease Relevance 0 Pain Relevance 0
Here, we describe the use of various fluorescently tagged G protein subunits and methods for using translocation and FRET-based G protein sensors in studying GPCR activation in living cells.
Positive_regulation (activation) of GPCR
4) Confidence 0.45 Published 2010 Journal Methods Mol. Biol. Section Abstract Doc Link 20336424 Disease Relevance 0.16 Pain Relevance 0.35
The ability of morphine to alleviate pain is mediated through a heterotrimeric guanine nucleotide binding protein (G protein)-coupled heptahelical receptor (GPCR), the mu opioid receptor (muOR).
Positive_regulation (mediated) of GPCR associated with pain, mu opioid receptor and morphine
5) Confidence 0.44 Published 1999 Journal Science Section Abstract Doc Link 10617462 Disease Relevance 0.10 Pain Relevance 0.53
Stimulation of a GPCR by an extracellular messenger, either physiological or synthetic, triggers intracellular receptor signaling via heterotrimeric G proteins.
Positive_regulation (Stimulation) of GPCR
6) Confidence 0.24 Published 2009 Journal PLoS ONE Section Body Doc Link PMC2672171 Disease Relevance 0 Pain Relevance 0.06
Stimulation of a GPCR by an extracellular ligand triggers receptor signaling via G proteins, and this process is highly regulated.
Positive_regulation (Stimulation) of GPCR
7) Confidence 0.24 Published 2009 Journal PLoS ONE Section Abstract Doc Link PMC2672171 Disease Relevance 0 Pain Relevance 0.12
This review gives an overview of current computational approaches to GPCR model building; ligand-receptor interaction for drug design; and molecular mechanism of GPCR activation from simulation.
Positive_regulation (activation) of GPCR
8) Confidence 0.24 Published 2010 Journal Curr. Med. Chem. Section Abstract Doc Link 20158474 Disease Relevance 0.14 Pain Relevance 0.07
CRF1 is a GPCR that is positively linked to the activation of AC and other second messenger systems such as IP3 and PKC (Bajo et al., 2008).
Positive_regulation (linked) of GPCR
9) Confidence 0.19 Published 2011 Journal Frontiers in Neuroscience Section Body Doc Link PMC3024005 Disease Relevance 0.37 Pain Relevance 0.33
The 5-HT2C subtype of the serotonin receptor family is a G-protein coupled receptor (GPCR) that is broadly expressed in the brain and is proposed to mediate many of the central nervous system actions of serotonin, including those underlying the therapeutic benefit of SSRI treatment in OCD [15].
Positive_regulation (proposed) of GPCR in central nervous system associated with anxiety disorder, central nervous system, ssri and serotonin
10) Confidence 0.17 Published 2008 Journal Current Chemical Genomics Section Body Doc Link PMC2746669 Disease Relevance 0.94 Pain Relevance 0.24
The CRF1 receptor is a G-protein-coupled receptor (GPCR) that is predominantly linked to the activation of adenylyl cyclase (AC), and also other second messenger systems such as inositol trisphosphate and protein kinase C (PKC; Grammatopoulos et al., 2001; Blank et al., 2003).
Positive_regulation (linked) of GPCR associated with kinase c
11) Confidence 0.16 Published 2011 Journal Frontiers in Neuroscience Section Body Doc Link PMC3024005 Disease Relevance 0.18 Pain Relevance 0.43
Also, we have recently shown that in prostate cancer cells, the pro-apoptotic Bcl-2 protein BAD plays a unique role as a convergence point of several anti-apoptotic signaling pathways that include constitutively active PI3K, activated EGFR and GPCR [6].
Positive_regulation (activated) of GPCR associated with prostate cancer and apoptosis
12) Confidence 0.15 Published 2009 Journal PLoS ONE Section Body Doc Link PMC2704953 Disease Relevance 1.58 Pain Relevance 0.12
However, the progression of each of these downstream events after GPCR stimulation depends first on the tyrosine phosphorylation of a membrane-bound protein that will be used as a scaffold, which will bind the other proteins (e.g.
Positive_regulation (stimulation) of GPCR
13) Confidence 0.14 Published 2002 Journal BMC Pharmacol Section Body Doc Link PMC88976 Disease Relevance 0 Pain Relevance 0
This similarity prompted us to confirm that farnesyl mono- and diphosphate activate various LPA GPCR targets (Liliom et al., 2006).
Positive_regulation (activate) of GPCR
14) Confidence 0.12 Published 2010 Journal British Journal of Pharmacology Section Body Doc Link PMC2989581 Disease Relevance 0.15 Pain Relevance 0.29
In search of the minimal pharmacophore that activates LPA GPCR, we identified fatty alcohol phosphates that, depending on the length of the hydrocarbon chain and the headgroup (phosphate or thiophosphate), function as either antagonists or agonists (Durgam et al., 2005; Deng et al., 2007; Zhang et al., 2009a).
Positive_regulation (activates) of GPCR associated with antagonist, agonist and alcohol
15) Confidence 0.12 Published 2010 Journal British Journal of Pharmacology Section Body Doc Link PMC2989581 Disease Relevance 0.18 Pain Relevance 0.26
Whereas LPA GPCR are activated by both saturated and unsaturated fatty acid-substituted LPAs, PPAR?
Positive_regulation (activated) of GPCR
16) Confidence 0.12 Published 2010 Journal British Journal of Pharmacology Section Body Doc Link PMC2989581 Disease Relevance 0.54 Pain Relevance 0.16
Thus, increased levels of several growth factors, including FGF, EGF, IL-6 and GPCR agonists that activate anti-apoptotic signaling pathways, have been reported in androgen-independent prostate cancer [3]–[7].
Positive_regulation (increased) of GPCR associated with agonist, prostate cancer and apoptosis
17) Confidence 0.11 Published 2009 Journal PLoS ONE Section Body Doc Link PMC2704953 Disease Relevance 1.40 Pain Relevance 0.05
Finally, the difficulty of monitoring the concentrations of endogenous ligands in the tissue of interest has complicated the interpretation of the studies of GPCR activation in vivo.
Positive_regulation (activation) of GPCR
18) Confidence 0.09 Published 2007 Journal PLoS ONE Section Body Doc Link PMC1930153 Disease Relevance 0 Pain Relevance 0.04
Thus, the ability to modulate basal signaling offers a unique opportunity to separate the physiological contribution of basal signaling versus ligand-mediated GPCR activation in vivo.
Positive_regulation (activation) of GPCR
19) Confidence 0.09 Published 2007 Journal PLoS ONE Section Body Doc Link PMC1930153 Disease Relevance 0.27 Pain Relevance 0.06
(Zhang et al., 2009a) have developed alpha-bromophosphonate analogues of LPA that inhibit ATX activity and also are antagonists of LPA1,2,3,4,5 GPCR and showed that these dual-action compounds not only reduce breast cancer metastasis but also inhibit tumour growth.
Positive_regulation (antagonists) of GPCR associated with cancer, antagonist, breast cancer and metastasis
20) Confidence 0.09 Published 2010 Journal British Journal of Pharmacology Section Body Doc Link PMC2989581 Disease Relevance 0.96 Pain Relevance 0.08

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