INT12129

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Context Info
Confidence 0.78
First Reported 1990
Last Reported 2010
Negated 5
Speculated 5
Reported most in Abstract
Documents 107
Total Number 112
Disease Relevance 23.11
Pain Relevance 27.60

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small molecule metabolic process (CYP3A4) oxidoreductase activity (CYP3A4) endoplasmic reticulum (CYP3A4)
enzyme binding (CYP3A4) lipid metabolic process (CYP3A4) cytoplasm (CYP3A4)
Anatomy Link Frequency
liver 25
PB-1 3
intestine 3
plasma 2
hepatocytes 2
CYP3A4 (Homo sapiens)
Pain Link Frequency Relevance Heat
fibrosis 27 99.92 Very High Very High Very High
Buprenorphine 579 99.80 Very High Very High Very High
methadone 380 99.80 Very High Very High Very High
Versed 133 99.60 Very High Very High Very High
Duloxetine 150 99.36 Very High Very High Very High
lidocaine 75 99.12 Very High Very High Very High
rapifen 52 99.06 Very High Very High Very High
Morphine 101 99.04 Very High Very High Very High
Inflammation 299 98.92 Very High Very High Very High
ketamine 29 98.88 Very High Very High Very High
Disease Link Frequency Relevance Heat
Sprains And Strains 57 99.98 Very High Very High Very High
Cirrhosis 206 99.92 Very High Very High Very High
Targeted Disruption 266 99.88 Very High Very High Very High
Cancer 385 99.64 Very High Very High Very High
Nicotine Addiction 145 99.56 Very High Very High Very High
Rickets 120 99.32 Very High Very High Very High
Nash(non-alcoholic Steatohepatitis) 27 99.20 Very High Very High Very High
INFLAMMATION 239 98.92 Very High Very High Very High
Nephrotoxicity 10 98.82 Very High Very High Very High
Toxicity 324 98.56 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Compared to reversible inhibition, mechanism-based inhibitors of CYP3A4 more frequently cause unfavorable drug-drug interactions, as the inactivated CYP3A4 has to be replaced by newly synthesized CYP3A4 protein.
Gene_expression (synthesized) of CYP3A4
1) Confidence 0.78 Published 2004 Journal Curr. Drug Metab. Section Abstract Doc Link 15544435 Disease Relevance 0.08 Pain Relevance 0.16
Compared with reversible inhibition of CYP3A4, mechanism-based inhibitors of CYP3A4 more frequently cause pharmacokinetic-pharmacodynamic drug–drug interactions, as the inactivated CYP3A4 has to be replaced by newly synthesized CYP3A4 protein.
Gene_expression (synthesized) of CYP3A4
2) Confidence 0.78 Published 2005 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC1661603 Disease Relevance 0 Pain Relevance 0.04
The expression of CYP3A can also be influenced by inflammation and proinflammatory cytokines, which are known to affect drug metabolism by downregulating or upregulating expression of several CYPs, including the CYP3A subfamily.
Gene_expression (expression) of CYP3A associated with inflammation and cytokine
3) Confidence 0.78 Published 2005 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC1661603 Disease Relevance 0.29 Pain Relevance 0.20
This is mainly due to the significant differences in the hepatic expression of CYP3A4, based on both in vitro (35–100-fold) studies with a human liver bank (Shimada et al 1994) and in vivo (20–50-fold) studies with probe drugs such as erythromycin (Watkins 1994), midazolam (Thummel et al 1994), and alfentanil (Kharasch et al 2003).
Gene_expression (expression) of CYP3A4 in liver associated with rapifen and versed
4) Confidence 0.78 Published 2005 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC1661603 Disease Relevance 0.29 Pain Relevance 0.25
Significant interindividual variability in the expression and activity of CYP3A4 has also been observed (Shimada et al 1994; Thummel et al 1994; von Richter et al 2004; Watanabe et al 2004).
Gene_expression (expression) of CYP3A4
5) Confidence 0.78 Published 2005 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC1661603 Disease Relevance 0 Pain Relevance 0.07
However, it appears that there are no marked age and gender differences in CYP3A4 expression (Hunt et al 1992; Schmucker 2001; Meibohm et al 2002), although 24%–36% higher activity in females has been reported (Watkins et al 1989).
Gene_expression (expression) of CYP3A4
6) Confidence 0.78 Published 2005 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC1661603 Disease Relevance 0.23 Pain Relevance 0.18
Importantly, mechanism-based CYP3A4 inactivation causes long-term effects on drug pharmacokinetics, as the inactivated CYP3A4 has to be replaced by newly synthesized CYP3A4 protein.
Gene_expression (synthesized) of CYP3A4
7) Confidence 0.78 Published 2005 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC1661603 Disease Relevance 0.09 Pain Relevance 0
HepG2 cell lines that constitutively and stably express human CYP3A4 were constructed in order to study enzyme interactions with CYP3A4 as the only P450 present.
Gene_expression (express) of CYP3A4
8) Confidence 0.78 Published 2002 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 11811955 Disease Relevance 0 Pain Relevance 0.37
The aims were to attest whether HepG2-GS-3A4, a cell line into which the human CYP3A4 gene was introduced, can be used for a screening of chemicals that will inhibit CYP3A4 activity. 2.
Gene_expression (introduced) of CYP3A4
9) Confidence 0.77 Published 2008 Journal Xenobiotica Section Abstract Doc Link 18846481 Disease Relevance 0 Pain Relevance 0.06
Since they are administered orally, and CYP3A4 is expressed in human intestine, we tested the hypotheses that human intestine can metabolize methadone and LAAM, and evaluated the participation of CYP3A4.
Gene_expression (expressed) of CYP3A4 in intestine associated with methadone
10) Confidence 0.77 Published 2001 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 11504799 Disease Relevance 0 Pain Relevance 0.85
N-Demethylation of LAAM and nor-LAAM by expressed CYP3A4 was unusual, with hyperbolic velocity curves and Eadie-Hofstee plots and without evidence of positive cooperativity.
Gene_expression (expressed) of CYP3A4
11) Confidence 0.76 Published 2001 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 11259570 Disease Relevance 0 Pain Relevance 0.21
Among the 13 P450 isoforms tested, CYP 3A4, 2C8, 3A5, and 3A7 produced Nor-BUP.
Gene_expression (produced) of CYP 3A4 in 3A5 associated with buprenorphine
12) Confidence 0.75 Published 2005 Journal Drug Metab. Dispos. Section Abstract Doc Link 15743975 Disease Relevance 0 Pain Relevance 1.46
The maximum rate of formation of D-617 and norverapamil was determined in the microsomal fraction of 21 human livers which had been previously characterized for the individual expression of various P450 enzymes (CYP1A2, CYP2C, CYP2D6, CYP2E1 and CYP3A3/4) by means of Western blotting.
Gene_expression (expression) of CYP3A in livers
13) Confidence 0.75 Published 1993 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 8232610 Disease Relevance 0.13 Pain Relevance 0.10
The availability of recently developed host cells that simultaneously overexpress yeast NADPH-P450 reductase and/or express human liver cytochrome b5, obtained through stable integration of the corresponding coding sequences into the yeast genome, led to biotechnological systems with much higher activities of yeast-expressed P450 NF25 and with much better ability to form P450 NF25-iron-metabolite complexes. 9-fold, 8-fold, and 30-fold rate increases were found respectively for nifedipine 1,4-oxidation, lidocaine N-deethylation and testosterone 6 beta-hydroxylation between P450 NF25-containing yeast microsomes from the basic strain and from the strain that both overexpresses yeast NADPH-P450 reductase and expresses human cytochrome b5.
Gene_expression (expressed) of NF25 in liver associated with sprains and strains and lidocaine
14) Confidence 0.75 Published 1992 Journal Eur. J. Biochem. Section Abstract Doc Link 1628642 Disease Relevance 0.18 Pain Relevance 0.09
It is unclear whether various natural and synthetic retinoids can regulate the expression of CYP3A4.
Gene_expression (expression) of CYP3A4
15) Confidence 0.75 Published 2006 Journal Toxicol. Sci. Section Abstract Doc Link 16632523 Disease Relevance 0.35 Pain Relevance 0.03
Taken together, retinoids activate the RXR/SXR-mediated pathway and regulate the expression of CYP3A4.
Gene_expression (expression) of CYP3A4
16) Confidence 0.75 Published 2006 Journal Toxicol. Sci. Section Abstract Doc Link 16632523 Disease Relevance 0.59 Pain Relevance 0.31
The effects of P450 isozymes on the kinetic parameters of UGT2B7-catalyzed glucuronidation of the morphine 3-hydroxyl group were examined by simultaneous expression of UGT2B7 and either CYP3A4, -1A2, or -2C9 in COS-1 cells.
Spec (examined) Gene_expression (expression) of CYP3A4 in 1A2 associated with morphine
17) Confidence 0.74 Published 2005 Journal Mol. Pharmacol. Section Abstract Doc Link 15611481 Disease Relevance 0 Pain Relevance 0.27
Although coexpression of CYP3A4 with UGT2B7 had little effect on Vmax, the Km was increased by about 9.8-fold compared with the UGT2B7 single expression system.
Gene_expression (coexpression) of CYP3A4
18) Confidence 0.74 Published 2005 Journal Mol. Pharmacol. Section Abstract Doc Link 15611481 Disease Relevance 0 Pain Relevance 0.31
Consequently, ketamine-caused cytoskeletal interruption led to suppression of CYP3A4 expression and its metabolizing activity.
Gene_expression (expression) of CYP3A4 associated with ketamine
19) Confidence 0.74 Published 2009 Journal Drug Metab. Dispos. Section Abstract Doc Link 18845661 Disease Relevance 0.14 Pain Relevance 0.50
We found that incubating transfected HepG2 cells that express CYP3A4 or a reconstituted microsomal model containing human liver microsomes and cytosol, high concentrations of acetaminophen could induce a dose- and time-dependent degradation of CYP3A4.
Gene_expression (express) of CYP3A4 in liver associated with paracetamol
20) Confidence 0.73 Published 2004 Journal Basic Clin. Pharmacol. Toxicol. Section Abstract Doc Link 15078344 Disease Relevance 0 Pain Relevance 0.33

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