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Literature summary for 2.4.1.17 extracted from

  • Benoit-Biancamano, M.O.; Connelly, J.; Villeneuve, L.; Caron, P.; Guillemette, C.
    Deferiprone glucuronidation by human tissues and recombinant UDP glucuronosyltransferase 1A6: an in vitro investigation of genetic and splice variants (2009), Drug Metab. Dispos., 37, 322-329.
    View publication on PubMed
Search for more literature for 2.4.1.17

Application

Application Comment Organism
medicine the UGT1A6 splice variant isoform 2, detected in the liver and kidney, has no transferase activity for deferiprone. When UGT1A6_i2 is coexpressed with the classic UGT1A6_i1 isoform, velocity is reduced for deferiprone but remains similar for 4-nitrophenol or serotonin glucuronidation Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information genetic variants UGT1A6*2 with residues A7A181S184, UGT1A6*3 with residue A7, UGT1A6*4 with residues A7S184, and UGT1A6*5 with resiude A181 show Km values similar to reference variant UGT1A6*1, but their Vmax values are reduced by 25% to 70% Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-nitrophenol competitive Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.73
-
 4-nitrophenol pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2 Homo sapiens
0.77
-
 4-nitrophenol pH 7.5, 37°C, genetic variant UGT1A6*1 Homo sapiens
7.4
-
 deferiprone pH 7.5, 37°C, genetic variant UGT1A6*3 Homo sapiens
8.2
-
 deferiprone pH 7.5, 37°C, genetic variant UGT1A6*2 Homo sapiens
8.2
-
 deferiprone pH 7.5, 37°C, genetic variant UGT1A6*4 Homo sapiens
8.2
-
 deferiprone pH 7.5, 37°C, genetic variant UGT1A6*5 Homo sapiens
9.8
-
 serotonin pH 7.5, 37°C, genetic variant UGT1A6*1 Homo sapiens
9.9
-
 serotonin pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2 Homo sapiens
10
-
 deferiprone pH 7.5, 37°C, genetic variant UGT1A6*1 Homo sapiens
19.3
-
 deferiprone pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2 Homo sapiens

Localization

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isoform UGT1A6
-

Source Tissue

Source Tissue Comment Organism Textmining
ileum
-
 Homo sapiens
-
jejunum
-
 Homo sapiens
-
kidney
-
 Homo sapiens
-
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenol + UDP-glucuronate
-
 Homo sapiens 4-nitrophenyl beta-D-glucuronide + UDP
-
 ?
deferiprone + UDP-glucuronate
-
 Homo sapiens deferiprone 3-O-glucuronide + UDP
-
 ?
serotonin + UDP-glucuronate
-
 Homo sapiens UDP + 3-(2-aminoethyl)-1H-indol-5-yl beta-D-glucuronide
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
23.4
-
 4-nitrophenol pH 7.5, 37°C, genetic variant UGT1A6*1 Homo sapiens
51.2
-
 4-nitrophenol pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2 Homo sapiens