INT64563

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Context Info
Confidence 0.75
First Reported 1996
Last Reported 2010
Negated 1
Speculated 4
Reported most in Abstract
Documents 27
Total Number 31
Disease Relevance 3.31
Pain Relevance 13.43

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

small molecule metabolic process (UGT1A1) endoplasmic reticulum (UGT1A1) enzyme binding (UGT1A1)
Anatomy Link Frequency
liver 4
astrocytes 2
intestine 2
plasma 1
hepatocytes 1
UGT1A1 (Homo sapiens)
Pain Link Frequency Relevance Heat
Morphine 552 100.00 Very High Very High Very High
Buprenorphine 45 99.96 Very High Very High Very High
Opioid 18 99.68 Very High Very High Very High
Paracetamol 24 98.44 Very High Very High Very High
Bile 49 97.24 Very High Very High Very High
MU agonist 3 96.20 Very High Very High Very High
antagonist 12 95.92 Very High Very High Very High
cINOD 10 92.48 High High
opioid receptor 42 81.16 Quite High
Catecholamine 17 79.88 Quite High
Disease Link Frequency Relevance Heat
Hemolysis 1 99.56 Very High Very High Very High
Liver Disease 3 98.80 Very High Very High Very High
Syndrome 13 98.36 Very High Very High Very High
Jaundice 6 97.84 Very High Very High Very High
Hyperbilirubinemia 27 97.52 Very High Very High Very High
Targeted Disruption 10 92.08 High High
Pancreatitis 3 87.40 High High
Van Bogaert's Disease 35 83.68 Quite High
Toxicity 31 80.72 Quite High
Pain 5 78.68 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
RT-PCR analysis demonstrated that the UGT1A isoforms, UGT1A3, 1A8, and 1A10, and UGT2B7 were expressed in the GI tract.
Gene_expression (expressed) of UGT1A
1) Confidence 0.75 Published 2004 Journal Biochim. Biophys. Acta Section Abstract Doc Link 15535975 Disease Relevance 0.15 Pain Relevance 0.64
Enzymes such as those in the UGT1A family, implicated in converting morphine to inactive M3G, are expressed in rat primary neurons and astrocytes [19].
Gene_expression (expressed) of UGT1A in astrocytes associated with morphine
2) Confidence 0.75 Published 2008 Journal PLoS ONE Section Body Doc Link PMC2265639 Disease Relevance 0.28 Pain Relevance 0.97
Pancreatic expression of UGT1A genes was identified by duplex reverse-transcription PCR.
Gene_expression (expression) of UGT1A
3) Confidence 0.75 Published 2003 Journal Gastroenterology Section Body Doc Link 12806614 Disease Relevance 0.09 Pain Relevance 0
The present study was designed to study the kinetic interaction of expressed human UGT2B7(Y) or (H), UGT1A1, and UGT1A3 toward 2- and 4-hydroxycatechol estrogens. cDNAs encoding UGT2B7(Y) or (H), UGT1A1, and UGT1A3 were expressed in HK293 cells, and cell homogenates or membrane preparations were used to determine their glucuronidation ability.
Gene_expression (expressed) of UGT1A1
4) Confidence 0.75 Published 1998 Journal Toxicol. Sci. Section Abstract Doc Link 9848110 Disease Relevance 0 Pain Relevance 0.15
The present study was designed to study the kinetic interaction of expressed human UGT2B7(Y) or (H), UGT1A1, and UGT1A3 toward 2- and 4-hydroxycatechol estrogens. cDNAs encoding UGT2B7(Y) or (H), UGT1A1, and UGT1A3 were expressed in HK293 cells, and cell homogenates or membrane preparations were used to determine their glucuronidation ability.
Gene_expression (expressed) of UGT1A1
5) Confidence 0.75 Published 1998 Journal Toxicol. Sci. Section Abstract Doc Link 9848110 Disease Relevance 0 Pain Relevance 0.26
The intestinal apparent Km value for E3G formation was essentially identical to that seen in liver, consistent with intestinal UGT1A1 expression.
Gene_expression (expression) of UGT1A1 in liver
6) Confidence 0.68 Published 2000 Journal Pharmacogenetics Section Abstract Doc Link 11186135 Disease Relevance 0 Pain Relevance 0.14
Furthermore, to estimate the contribution of these UGT isozymes in M6G formation in vivo, the expression levels of UGT1A1 and 1A8 mRNA in human liver and intestine were determined by reverse transcription real-time polymerase chain reaction.
Spec (determined) Gene_expression (expression) of UGT1A1 in intestine
7) Confidence 0.67 Published 2008 Journal Drug Metab. Dispos. Section Abstract Doc Link 18187562 Disease Relevance 0 Pain Relevance 0.79
UGT1A1 was also predicted to contribute substantially at toxic concentrations (>1 mM; >28% activity), whereas UGT1A6 was most active at relatively low concentrations (<50 microM; >29% activity).
Gene_expression (active) of UGT1A1
8) Confidence 0.65 Published 2001 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 11714888 Disease Relevance 0 Pain Relevance 0.67
Other polymorphisms in the genes encoding for the UGT isoenzymes could also be associated with Gilbert’s syndrome.40,41 Lankisch et al examined the effects of different polymorphisms in UGT1A1 (UGT1A1*28), UGT1A3 (-66) and UGT1A7 (?
Gene_expression (isoenzymes) of UGT associated with syndrome
9) Confidence 0.65 Published 2009 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2697529 Disease Relevance 0.94 Pain Relevance 0
Using the RAF approach, we found that UGT1A1 and UGT2B7 accounted for approximately 10 and 41% of BUP glucuronidation, respectively.
Gene_expression (accounted) of UGT1A1 associated with buprenorphine
10) Confidence 0.62 Published 2010 Journal Drug Metab. Dispos. Section Abstract Doc Link 19841060 Disease Relevance 0 Pain Relevance 1.00
Among the six hepatic UGT isoforms tested, UGT1A1, UGT1A3, and UGT2B7 metabolized BUP and Nor-BUP.
Neg (Nor) Gene_expression (metabolized) of UGT1A1 associated with buprenorphine
11) Confidence 0.62 Published 2010 Journal Drug Metab. Dispos. Section Abstract Doc Link 19841060 Disease Relevance 0 Pain Relevance 1.00
Interestingly, enzymes implicated in converting morphine into M3G (i.e., UGT1A enzymes) are expressed in primary neurons [19] and astrocytes [63].
Gene_expression (expressed) of UGT1A in astrocytes associated with morphine
12) Confidence 0.58 Published 2008 Journal PLoS ONE Section Body Doc Link PMC2265639 Disease Relevance 0 Pain Relevance 1.19
The present study was designed to study the kinetic interaction of expressed human UGT2B7(Y) or (H), UGT1A1, and UGT1A3 toward 2- and 4-hydroxycatechol estrogens. cDNAs encoding UGT2B7(Y) or (H), UGT1A1, and UGT1A3 were expressed in HK293 cells, and cell homogenates or membrane preparations were used to determine their glucuronidation ability.
Gene_expression (expressed) of UGT1A1
13) Confidence 0.58 Published 1998 Journal Toxicol. Sci. Section Abstract Doc Link 9848110 Disease Relevance 0 Pain Relevance 0.26
The present study was designed to study the kinetic interaction of expressed human UGT2B7(Y) or (H), UGT1A1, and UGT1A3 toward 2- and 4-hydroxycatechol estrogens. cDNAs encoding UGT2B7(Y) or (H), UGT1A1, and UGT1A3 were expressed in HK293 cells, and cell homogenates or membrane preparations were used to determine their glucuronidation ability.
Gene_expression (expressed) of UGT1A1
14) Confidence 0.58 Published 1998 Journal Toxicol. Sci. Section Abstract Doc Link 9848110 Disease Relevance 0 Pain Relevance 0.26
Glucuronidation of 1'-HE was not detected in cells expressing UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A7, UGT1A8, and UGT1A10. 1'-HE glucuronidation in 27 individual human liver samples significantly (p < 0.05) correlated with the glucuronidation of other UGT2B7 substrates (morphine and ibuprofen).
Gene_expression (expressing) of UGT1A1 in liver associated with morphine
15) Confidence 0.56 Published 2003 Journal Toxicol. Sci. Section Abstract Doc Link 12657745 Disease Relevance 0 Pain Relevance 0.09
The human UGT superfamily is comprised of 2 families (UGT1 and UGT2) and 3 subfamilies (UGT1A, UGT2A, and UGT2B).
Gene_expression (comprised) of UGT1A
16) Confidence 0.55 Published 2005 Journal Pharmacol. Ther. Section Abstract Doc Link 15781124 Disease Relevance 0 Pain Relevance 0.05
The present study was designed to characterize the reactivity of expressed human UGT1.1 with opioid compounds and compare its substrate specificity for opioids to that of the expressed rat enzyme.
Gene_expression (expressed) of UGT1 associated with opioid
17) Confidence 0.55 Published 1996 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 8806713 Disease Relevance 0 Pain Relevance 0.67
We have previously shown that rat UGT1.1, stably expressed in human embryonic kidney 293 cells, catalyzes the glucuronidation of bilirubin and the mixed opioid agonist/antagonist buprenorphine with high efficiency.
Gene_expression (expressed) of UGT1 in embryonic kidney associated with mu agonist, antagonist and buprenorphine
18) Confidence 0.55 Published 1996 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 8806713 Disease Relevance 0 Pain Relevance 0.52
Furthermore, to estimate the contribution of these UGT isozymes in M6G formation in vivo, the expression levels of UGT1A1 and 1A8 mRNA in human liver and intestine were determined by reverse transcription real-time polymerase chain reaction.
Spec (determined) Gene_expression (levels) of UGT1A1 in intestine
19) Confidence 0.52 Published 2008 Journal Drug Metab. Dispos. Section Abstract Doc Link 18187562 Disease Relevance 0 Pain Relevance 0.78
Irreversible binding to cellular proteins in culture was also evident with the addition of mefenamic acid to the heterologous Chinese hamster lung fibroblast cell line V79 expressing the human UDP-glucuronosyltransferase isoenzyme UGT1*02.
Gene_expression (expressing) of UDP-glucuronosyltransferase isoenzyme UGT1 in fibroblast
20) Confidence 0.44 Published 1996 Journal Drug Metab. Dispos. Section Abstract Doc Link 8869817 Disease Relevance 0.05 Pain Relevance 0.05

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