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Literature summary for 2.4.1.17 extracted from

  • King, C.; Tang, W.; Ngui, J.; Tephly, T.; Braun, M.
    Characterization of rat and human UDP-glucuronosyltransferases responsible for the in vitro glucuronidation of diclofenac (2001), Toxicol. Sci., 61, 49-53.
    View publication on PubMed
Search for more literature for 2.4.1.17

Inhibitors

Inhibitors Comment Organism Structure
diclofenac inhibits the in vitro glucuronidation of morphine and codeine by liver microsomes Homo sapiens
Dihydrocodeine
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.007
-
 diclofenac UGT2B1 Rattus norvegicus
0.013
-
 diclofenac liver microsomes Rattus norvegicus
0.013
-
 diclofenac UGT2B7 Homo sapiens
0.016
-
 diclofenac
-
 Rattus norvegicus
0.016
-
 diclofenac UGT1A9 Homo sapiens
0.02
-
 diclofenac liver microsomes Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-
microsome
-
 Rattus norvegicus
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 overview
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-
liver
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
diclofenac + UDPalpha-D-glucuronate UGT2B7 active at high rate, recombinant UGT1A9 active at moderate rate, UGT1A6 and UGT2B15 active at low rates Homo sapiens UDP + ?
-
 ?
diclofenac + UDPalpha-D-glucuronate recombinant UGT2B1 displays moderate rate Rattus norvegicus UDP + ?
-
 ?
morphine + UDP-glucuronate substrate for UGT2B7 Homo sapiens UDP + morphine 3,6-diglucuronide
-
 ?
morphine + UDP-glucuronate substrate for UGT2B1 Rattus norvegicus UDP + morphine 3,6-diglucuronide
-
 ?
opiates + UDPglucuronate substrate for UGT2B7 Homo sapiens opiates 6-O-glucuronides + UDP
-
 ?