INT65880

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Context Info
Confidence 0.77
First Reported 1996
Last Reported 2010
Negated 2
Speculated 2
Reported most in Body
Documents 25
Total Number 27
Disease Relevance 9.49
Pain Relevance 1.92

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small molecule metabolic process (CYP2C8) endoplasmic reticulum (CYP2C8)
Anatomy Link Frequency
liver 5
tube 1
endothelial cells 1
monocyte 1
Caco-2 1
CYP2C8 (Homo sapiens)
Pain Link Frequency Relevance Heat
diclofenac 4 99.50 Very High Very High Very High
cINOD 7 97.96 Very High Very High Very High
rapifen 7 97.82 Very High Very High Very High
fluoxetine 3 94.56 High High
alcohol 2 94.12 High High
Dextromethorphan 1 93.80 High High
antagonist 30 93.36 High High
Versed 7 91.80 High High
Morphine 1 82.64 Quite High
Analgesic 5 75.00 Quite High
Disease Link Frequency Relevance Heat
Hepatotoxicity 8 99.96 Very High Very High Very High
Prostate Cancer 21 99.60 Very High Very High Very High
Genetic Predisposition To Disease 1 99.22 Very High Very High Very High
Cancer 367 99.00 Very High Very High Very High
Hypothermia 243 98.96 Very High Very High Very High
Nicotine Addiction 70 97.56 Very High Very High Very High
Malignant Neoplastic Disease 11 97.56 Very High Very High Very High
Arrhythmias 2 Under Development 5 97.36 Very High Very High Very High
INFLAMMATION 120 97.24 Very High Very High Very High
Reprotox - General 1 23 96.52 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Cytochrome P450 (CYP) superfamily members CYP2C8 and CYP2C9 are polymorphically expressed enzymes that are involved in the metabolic inactivation of several drugs, including, among others, antiepileptics, NSAIDs, oral hypoglycemics, and anticoagulants.
Gene_expression (expressed) of CYP2C8 associated with cinod
1) Confidence 0.77 Published 2006 Journal Molecular diagnosis & therapy Section Abstract Doc Link 16646575 Disease Relevance 0 Pain Relevance 0.10
These transformants are designated Hepc/1A1.4, Hepc/1A2.9, Hepc/2A6L.14, Hepc/2B6.68, Hepc/2C8.46, Hepc/2C9.1, Hepc/2C19.12, Hepc/2D6.39, Hepc/2E1.3-8 and Hepc/3A4.2-30, which stably expressed human CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4, respectively.
Gene_expression (expressed) of CYP2C8 in 1A2
2) Confidence 0.68 Published 2001 Journal Toxicol In Vitro Section Abstract Doc Link 11377097 Disease Relevance 0 Pain Relevance 0.05
The final set covered CYP2C8 from just upstream of the coding sequence to just shy of the last exon.
Gene_expression (covered) of CYP2C8
3) Confidence 0.67 Published 2009 Journal Pharmacogenomics J Section Body Doc Link PMC2782405 Disease Relevance 0 Pain Relevance 0
The three are CYP2C9*144Cys, CYP2C8*399Arg and CYP2C8*139Lys.
Gene_expression (144Cys) of CYP2C8
4) Confidence 0.67 Published 2009 Journal Pharmacogenomics J Section Body Doc Link PMC2782405 Disease Relevance 0.15 Pain Relevance 0
Although CYP2C8*399Arg and CYP2C8*139Lys are always seen in cis, they occur with the CYP2C9*144Cys variant in haplotype G and without it in haplotype K.
Gene_expression (399Arg) of CYP2C8
5) Confidence 0.67 Published 2009 Journal Pharmacogenomics J Section Body Doc Link PMC2782405 Disease Relevance 0.20 Pain Relevance 0
Although CYP2C8*399Arg and CYP2C8*139Lys are always seen in cis, they occur with the CYP2C9*144Cys variant in haplotype G and without it in haplotype K.
Gene_expression (seen) of CYP2C8
6) Confidence 0.67 Published 2009 Journal Pharmacogenomics J Section Body Doc Link PMC2782405 Disease Relevance 0.20 Pain Relevance 0
Finally, immunoquantitation revealed that in these human liver samples, expression of CYP2C9 (88. 5 +/- 36 nmol/mg) was 5-fold higher than that of CYP2C19 (17.8 +/- 14 nmol/mg) and nearly 8-fold higher than that of CYP2C8 (11.5 +/- 12 nmol/mg).
Gene_expression (expression) of CYP2C8 in liver
7) Confidence 0.67 Published 1998 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 9578596 Disease Relevance 0 Pain Relevance 0
Direct (IC(50), K(i)) and time-dependent inhibition (IC(50) shift, K(I)/k(inact)) assays were validated in human liver microsomes with liquid chromatography-tandem mass spectrometry (LC/MS/MS) analysis for the following enzyme/substrate/inhibitor combinations: CYP1A2/phenacetin/alpha-naphthoflavone/furafylline, CYP2C8/amodiaquine/montelukast/gemfibrozil-1-O-beta-glucuronide, CYP2C9/diclofenac/sulfaphenazole/tienilic acid, CYP2C19/S-mephenytoin/S-benzylnirvanol/S-fluoxetine, CYP2D6/dextromethorphan/quinidine/paroxetine, and CYP3A4/midazolam/testosterone/ketoconazole/azamulin/verapamil/diltiazem.
Gene_expression (amodiaquine) of CYP2C8 in liver associated with versed, dextromethorphan, diclofenac and fluoxetine
8) Confidence 0.65 Published 2009 Journal Xenobiotica Section Abstract Doc Link 19255936 Disease Relevance 0 Pain Relevance 0.24
Though our retrospective investigation did not find the same association between the CYP2C8 rs1934951 SNP and the development ONJ as Sarasquete et al,25 more studies in independent patient cohorts are necessary to determine if genetic polymorphisms in CYP2C8 are a risk factor for the development of ONJ.
Gene_expression (rs1934951) of CYP2C8
9) Confidence 0.64 Published 2010 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2999510 Disease Relevance 0.26 Pain Relevance 0
DMO production by human cDNA expressed CYP enzymes was observed mainly for CYP2E1 (10.8 nmol/tube), marginally for CYP2C8 (0.22 nmol/tube) and not detectable for other CYP enzymes. 4.
Neg (not) Gene_expression (detectable) of CYP2C8 in tube
10) Confidence 0.62 Published 1998 Journal Xenobiotica Section Abstract Doc Link 9879636 Disease Relevance 0 Pain Relevance 0.07
Furthermore, rates of norfentanyl production by 10 individual human liver samples were highly correlated (r2 = 0.876, F = 56.46 p < 0.001) with immunochemically determined levels of CYP3A4 present in the samples but not with levels of CYP2C8, CYP2C9, CYP2C19, or CYP2E1.
Neg (not) Gene_expression (present) of CYP2C8 in liver
11) Confidence 0.61 Published 1996 Journal Drug Metab. Dispos. Section Abstract Doc Link 8886601 Disease Relevance 0 Pain Relevance 0.33
Expression of CYP1A2, CYP2C8, CYP2C18, CYP2C19, CYP2D6, CYP3A7, CYP4A11, FMO1, and FMO3 was below the limit of detection (LOD) in all investigated samples (data not shown).


Spec (investigated) Gene_expression (Expression) of CYP2C8
12) Confidence 0.56 Published 2006 Journal Environ Health Perspect Section Body Doc Link PMC1665420 Disease Relevance 0.48 Pain Relevance 0
4) including genes that metabolize xenobiotics and drugs (e.g., SULT1C3, UGT2B7, and CYP2C8).
Gene_expression (e.g.) of CYP2C8
13) Confidence 0.54 Published 2008 Journal PLoS Genetics Section Body Doc Link PMC2483296 Disease Relevance 0.33 Pain Relevance 0.06
Microsomes prepared from different human liver samples were compared for their abilities to metabolize fentanyl, sufentanil and alfentanil, and it was found that disappearance of the three substrates was well correlated with immunoreactive CYP3A4 contents but not with other CYPs, including CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6 and CYP2E1.
Gene_expression (contents) of CYP2C8 in liver associated with rapifen
14) Confidence 0.50 Published 1997 Journal Biochem. Pharmacol. Section Abstract Doc Link 9264313 Disease Relevance 0 Pain Relevance 0.38
Selected compounds were screened for cytochrome P450 inhibition (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4), metabolic stability (rat and human liver microsomes), and cell-membrane permeability (Caco-2).
Gene_expression (screened) of CYP2C8 in Caco-2
15) Confidence 0.41 Published 2006 Journal ChemMedChem Section Abstract Doc Link 16892345 Disease Relevance 0 Pain Relevance 0.10
METHODS: BUP was incubated with psychotropic drugs and cDNA-expressed CYP 3A4 and CYP 2C8 enzymes.
Gene_expression (cDNA-expressed) of CYP 2C8
16) Confidence 0.40 Published 2006 Journal Eur. J. Clin. Pharmacol. Section Body Doc Link 16802166 Disease Relevance 0 Pain Relevance 0
Genetic susceptibility to diclofenac-induced hepatotoxicity: contribution of UGT2B7, CYP2C8, and ABCC2 genotypes.
Gene_expression (contribution) of CYP2C8 associated with genetic predisposition to disease, hepatotoxicity and diclofenac
17) Confidence 0.38 Published 2007 Journal Gastroenterology Section Title Doc Link 17241877 Disease Relevance 0.57 Pain Relevance 0.24
Enayetallah et al. analyzed three cytochrome P450 epoxygenases (CYP2C8, CYP2C9, and CYP2J2) and soluble epoxide hydrolase in human malignant neoplasms [127].
Spec (analyzed) Gene_expression (analyzed) of CYP2C8 associated with malignant neoplastic disease
18) Confidence 0.34 Published 2010 Journal Cancer Metastasis Rev Section Body Doc Link PMC2962793 Disease Relevance 1.31 Pain Relevance 0
For instance, CYP2C8, CYP2C9, and CYP2J2 were recently shown to be expressed in three prostate carcinoma cell lines (PC3, DU-145, and LNCaP) [125].
Gene_expression (expressed) of CYP2C8 associated with prostate cancer
19) Confidence 0.30 Published 2010 Journal Cancer Metastasis Rev Section Body Doc Link PMC2962793 Disease Relevance 1.37 Pain Relevance 0.09
In turn, VEGF can increase CYP2C promoter activity in endothelial cells and induce the expression of CYP2C8, resulting in increased intracellular EET levels [115].
Gene_expression (expression) of CYP2C8 in endothelial cells
20) Confidence 0.30 Published 2010 Journal Cancer Metastasis Rev Section Body Doc Link PMC2962793 Disease Relevance 0.55 Pain Relevance 0.09

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