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Literature summary extracted from

  • Miners, J.O.; Chau, N.; Rowland, A.; Burns, K.; McKinnon, R.A.; Mackenzie, P.I.; Tucker, G.T.; Knights, K.M.; Kichenadasse, G.
    Inhibition of human UDP-glucuronosyltransferase enzymes by lapatinib, pazopanib, regorafenib and sorafenib Implications for hyperbilirubinemia (2017), Biochem. Pharmacol., 129, 85-95 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 expressed in HEK-293 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 lapatinib
-
 Homo sapiens
2.4.1.17 additional information isoforms UGT2B4, UGT2B7, UGT2B15 and UGT2B17 are not inhibited by lapatinib. Isoforms UGT2B4 and UGT2B17 are not inhibited by pazopanib. Isoforms UGT2B4 and UGT2B15 are not inhibited by regorafenib Homo sapiens
2.4.1.17 pazopanib
-
 Homo sapiens
2.4.1.17 regorafenib
-
 Homo sapiens
2.4.1.17 sorafenib
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
 Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.4.1.17 Mg2+ 4 mM used in assay conditions Homo sapiens

Organism

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

Source Tissue

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 4-methylumbelliferone + UDP-glucuronate
-
 Homo sapiens UDP + 4-methylumbelliferyl-beta-D-glucuronide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase
-
 Homo sapiens
2.4.1.17 UGT 1A10 isoform Homo sapiens
2.4.1.17 UGT 1A3 isoform Homo sapiens
2.4.1.17 UGT 1A4 isoform Homo sapiens
2.4.1.17 UGT 1A6 isoform Homo sapiens
2.4.1.17 UGT 1A7 isoform Homo sapiens
2.4.1.17 UGT 1A8 isoform Homo sapiens
2.4.1.17 UGT 1A9 isoform Homo sapiens
2.4.1.17 UGT 2B15 isoform Homo sapiens
2.4.1.17 UGT 2B17 isoform Homo sapiens
2.4.1.17 UGT 2B4 isoform Homo sapiens
2.4.1.17 UGT 2B7 isoform Homo sapiens
2.4.1.17 UGT1A1 isoform Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 0.000045
-
 isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.000066
-
 isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.000187
-
 isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.000261
-
 isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.000306
-
 isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.000317
-
 isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.000383
-
 isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.000536
-
 isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens lapatinib
2.4.1.17 0.000805
-
 isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.0011
-
 isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.0011
-
 isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens lapatinib
2.4.1.17 0.0011
-
 isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens lapatinib
2.4.1.17 0.0015
-
 isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens lapatinib
2.4.1.17 0.00159
-
 isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.002
-
 isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.0023
-
 isoform UGT1A3, at pH 7.4, temperature not specified in the publication Homo sapiens lapatinib
2.4.1.17 0.0034
-
 isoform UGT1A6, at pH 7.4, temperature not specified in the publication Homo sapiens lapatinib
2.4.1.17 0.0035
-
 isoform UGT1A6, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.0039
-
 isoform UGT1A6, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.0042
-
 isoform UGT1A6, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.0052
-
 isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.0075
-
 isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.0076
-
 isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.0082
-
 isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens lapatinib
2.4.1.17 0.0085
-
 isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.0092
-
 isoform UGT1A4, at pH 7.4, temperature not specified in the publication Homo sapiens lapatinib
2.4.1.17 0.0113
-
 isoform UGT1A4, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.016
-
 isoform UGT1A4, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.0161
-
 isoform UGT1A4, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.0193
-
 isoform UGT1A3, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.0198
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.0215
-
 isoform UGT2B17, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.0273
-
 isoform UGT1A3, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.0355
-
 isoform UGT1A3, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.0391
-
 isoform UGT2B17, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib
2.4.1.17 0.0442
-
 isoform UGT2B15, at pH 7.4, temperature not specified in the publication Homo sapiens pazopanib
2.4.1.17 0.0522
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.0544
-
 isoform UGT2B4, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.0587
-
 isoform UGT2B15, at pH 7.4, temperature not specified in the publication Homo sapiens sorafenib
2.4.1.17 0.0655
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens regorafenib