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Literature summary for 2.4.1.17 extracted from

  • Jinno, H.; Saeki, M.; Saito, Y.; Tanaka-Kagawa, T.; Hanioka, N.; Sai, K.; Kaniwa, N.; Ando, M.; Shirao, K.; Minami, H.; Ohtsu, A.; Yoshida, T.; Saijo, N.; Ozawa, S.; Sawada, J.
    Functional characterization of human UDP-glucuronosyltransferase 1A9 variant, D256N, found in Japanese cancer patients (2003), J. Pharmacol. Exp. Ther., 306, 688-693.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant D256N enzymes in COS-1 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information mutant isozyme UGT1A9 D256N is isolated from a japanese cancer patient, site-directed mutagenesis for expression plasmid construction, the mutant shows less than 5% of wild-type isozyme activity with 7-ethyl-10-hydroxycampothecin as substrate, the naturally occuring mutant isozyme might be involved in irinotecan metabolism in vivo Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
19.3
-
7-ethyl-10-hydroxycampothecin recombinant wild-type isozyme UGT1A9, pH.4, 37°C Homo sapiens
44.4
-
7-ethyl-10-hydroxycampothecin recombinant UGT1A9 mutant D256N isozyme, pH.4, 37°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O60656 isozymes UGT1A1, UGT1A7, UGT1A9, naturally occuring UGT1A9 mutant D256N, the latter from a japanese cancer patient
-

Source Tissue

Source Tissue Comment Organism Textmining
liver isozyme UGT1A1 and UGT1A9 Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information in contrast to isozymes UGT1A1 and UGT1A7, the isozyme UGT1A9 does not show polymorphism influencing the glucuronidation activity of SN-38 Homo sapiens ?
-
?
UDP-glucuronate + 7-ethyl-10-hydroxycampothecin i.e. SN-38, isozymes UGT1A1, UGT1A7, and UGT1A9 Homo sapiens UDP + 7-ethyl-10-hydroxycampothecin 1-O-beta-D-glucuronide
-
?

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase 1A9
-
Homo sapiens
UGT1A9
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens