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Literature summary for 2.4.1.17 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)

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

Inhibitors

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

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

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

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.
bilirubin + UDPglucuronate
-
Homo sapiens UDP + bilirubin O-glucuronide
-
?
bilirubin + UDPglucuronate
-
Rattus norvegicus UDP + bilirubin O-glucuronide
-
?
bilirubin + UDPglucuronate
-
Rattus norvegicus Gunn UDP + bilirubin O-glucuronide
-
?
bilirubin + UDPglucuronate
-
Rattus norvegicus Wistar UDP + bilirubin O-glucuronide
-
?
troglitazone + UDPglucuronate
-
Homo sapiens UDP + troglitazone 6-O-glucuronide
-
?
troglitazone + UDPglucuronate Gunn and Wistar strains Rattus norvegicus UDP + troglitazone 6-O-glucuronide
-
?
troglitazone + UDPglucuronate Gunn and Wistar strains Rattus norvegicus Gunn UDP + troglitazone 6-O-glucuronide
-
?
troglitazone + UDPglucuronate Gunn and Wistar strains Rattus norvegicus Wistar UDP + troglitazone 6-O-glucuronide
-
?

Ki Value [mM]

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