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Literature summary extracted from

  • Korprasertthaworn, P.; Rowland, A.; Lewis, B.C.; Mackenzie, P.I.; Yoovathaworn, K.; Miners, J.O.
    Effects of amino acid substitutions at positions 33 and 37 on UDP-glucuronosyltransferase 1A9 (UGT1A9) activity and substrate selectivity (2012), Biochem. Pharmacol., 84, 1511-1521.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 isoform UGT1A, expression in HEK-293T cell Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.4.1.17 H37L mutant of isoform UGT1A9, abolishes activity towards all substrates tested except retigabine Homo sapiens
2.4.1.17 H37P mutant of isoform UGT1A9, abolishes activity towards all substrates tested except retigabine Homo sapiens
2.4.1.17 H37Q mutant of isoform UGT1A9, abolishes activity towards all substrates tested except retigabine Homo sapiens
2.4.1.17 M33I mutant of isoform UGT1A9, increase in both Km and Vmax value Homo sapiens
2.4.1.17 M33Q mutant of isoform UGT1A9, increase in both Km and Vmax value Homo sapiens
2.4.1.17 M33T mutant of isoform UGT1A9, increase in both Km and Vmax value Homo sapiens
2.4.1.17 M33V mutant of isoform UGT1A9, increase in both Km and Vmax value Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.011
-
 4-methylumbeliferone wildtype, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.014
-
 sulfinpyrazone wildtype, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.0209
-
 frusemide mutant M33T, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.026
-
 propofol wildtype, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.032
-
 sulfinpyrazone mutant M33I, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.032
-
 retigabine wildtype, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.033
-
 sulfinpyrazone mutant M33Q, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.039
-
 sulfinpyrazone mutant M33V, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.046
-
 Mycophenolic acid mutant M33Q, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.053
-
 sulfinpyrazone mutant M33T, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.055
-
 retigabine mutant M33Q, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.062
-
 retigabine mutant M33V, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.068
-
 retigabine mutant M33T, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.07
-
 propofol mutant M33Q, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.087
-
 Mycophenolic acid wildtype, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.099
-
 retigabine mutant M33I, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.109
-
 propofol mutant M33V, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.113
-
 propofol mutant M33I, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.113
-
 propofol mutant M33T, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.129
-
 frusemide mutant M33V, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.157
-
 Mycophenolic acid mutant M33I, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.183
-
 frusemide mutant M33Q, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.187
-
 frusemide mutant M33I, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.2
-
 Mycophenolic acid mutant M33V, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.228
-
 4-methylumbeliferone mutant M33Q, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.229
-
 frusemide wildtype, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.233
-
 4-methylumbeliferone mutant M33I, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.234
-
 4-methylumbeliferone mutant M33V, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.336
-
 Mycophenolic acid mutant M33T, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.507
-
 (S)-naproxen mutant M33V, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.62
-
 (S)-naproxen mutant M33I, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.66
-
 (S)-naproxen mutant M33Q, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.79
-
 (S)-naproxen wildtype, pH 7.4, 37°C Homo sapiens
2.4.1.17 1.013
-
 (S)-naproxen mutant M33T, pH 7.4, 37°C Homo sapiens
2.4.1.17 1.621
-
 4-methylumbeliferone mutant M33T, pH 7.4, 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 (S)-naproxen + UDP-alpha-D-glucuronate
-
 Homo sapiens beta-D-glucuronosyl (S)-naproxen + UDP
-
 ?
2.4.1.17 4-methylumbeliferone + UDP-alpha-D-glucuronate
-
 Homo sapiens 4-methylumbelliferyl-7-O-alpha-D-glucuronide
-
 ?
2.4.1.17 frusemide + UDP-alpha-D-glucuronate
-
 Homo sapiens frusemide D-glucuronide
-
 ?
2.4.1.17 mycophenolic acid + UDP-alpha-D-glucuronate
-
 Homo sapiens mycophenolic acid D-glucuronide
-
 ?
2.4.1.17 propofol + UDP-alpha-D-glucuronate
-
 Homo sapiens UDP + propofol D-glucuronide
-
 ?
2.4.1.17 retigabine + UDP-alpha-D-glucuronate
-
 Homo sapiens retigabine D-glucuronide
-
 ?
2.4.1.17 sulfinpyrazone + UDP-alpha-D-glucuronate
-
 Homo sapiens sulfinpyrazone D-glucuronide
-
 ?