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Literature summary extracted from

  • Yoshigae, Y.; Konno, K.; Takasaki, W.; Ikeda, T.
    Characterization of UDP-glucuronosyltransferases (UGTS) involved in the metabolism of troglitazone in rats and humans (2000), J. Toxicol. Sci., 25, 433-441.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 expressed in baculovirus-infected insect cells and human B-lymphoblastoid cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 androsterone inhibition of glucuronidation of troglitazone catalyzed by isozymes of UGT2 family Homo sapiens
2.4.1.17 androsterone Gunn rat strain, competitive inhibition of troglitazone glucuronidation Rattus norvegicus
2.4.1.17 menthol Gunn rat, non-competitive inhibition of troglitazone glucuronidation Rattus norvegicus
2.4.1.17 testosterone inhibition of glucuronidation of troglitazone catalyzed by isozymes of UGT2 family, other 8 steroids tested on hUGT2A1 Homo sapiens
2.4.1.17 testosterone Gunn rat, non-competitive inhibition of troglitazone glucuronidation Rattus norvegicus
2.4.1.17 troglitazone inhibition of bilirubin glucuronidation by UGT1A1 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.136
-
troglitazone
-
Homo sapiens
2.4.1.17 0.136
-
troglitazone
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.1.17 bilirubin + UDPglucuronate Homo sapiens
-
UDP + bilirubin O-glucuronide
-
?
2.4.1.17 bilirubin + UDPglucuronate Rattus norvegicus
-
UDP + bilirubin O-glucuronide
-
?
2.4.1.17 bilirubin + UDPglucuronate Rattus norvegicus Gunn
-
UDP + bilirubin O-glucuronide
-
?
2.4.1.17 bilirubin + UDPglucuronate Rattus norvegicus Wistar
-
UDP + bilirubin O-glucuronide
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
-
-
2.4.1.17 Rattus norvegicus
-
Wistar strain
-
2.4.1.17 Rattus norvegicus
-
Gunn strain
-
2.4.1.17 Rattus norvegicus Gunn
-
Gunn strain
-
2.4.1.17 Rattus norvegicus Wistar
-
Wistar strain
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 liver
-
Homo sapiens
-
2.4.1.17 liver
-
Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 bilirubin + UDPglucuronate
-
Homo sapiens UDP + bilirubin O-glucuronide
-
?
2.4.1.17 bilirubin + UDPglucuronate
-
Rattus norvegicus UDP + bilirubin O-glucuronide
-
?
2.4.1.17 bilirubin + UDPglucuronate
-
Rattus norvegicus Gunn UDP + bilirubin O-glucuronide
-
?
2.4.1.17 bilirubin + UDPglucuronate
-
Rattus norvegicus Wistar UDP + bilirubin O-glucuronide
-
?
2.4.1.17 troglitazone + UDPglucuronate
-
Homo sapiens UDP + troglitazone 6-O-glucuronide
-
?
2.4.1.17 troglitazone + UDPglucuronate Gunn and Wistar strains Rattus norvegicus UDP + troglitazone 6-O-glucuronide
-
?
2.4.1.17 troglitazone + UDPglucuronate Gunn and Wistar strains Rattus norvegicus Gunn UDP + troglitazone 6-O-glucuronide
-
?
2.4.1.17 troglitazone + UDPglucuronate Gunn and Wistar strains Rattus norvegicus Wistar UDP + troglitazone 6-O-glucuronide
-
?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.009
-
androsterone Gunn rat, inhibition of troglitazone glucuronidation Rattus norvegicus
2.4.1.17 0.059
-
testosterone Gunn rat, inhibition of troglitazone glucuronidation Rattus norvegicus
2.4.1.17 0.112
-
testosterone inhibition of 2-hydroxyestradiol glucuronidation Homo sapiens
2.4.1.17 0.149
-
androsterone inhibition of troglitazone glucuronidation Homo sapiens