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Literature summary extracted from

  • Mroz, A.; Ryska, I.; Sominko, H.; Bejrowska, A.; Mazerska, Z.
    Drug-drug interaction potential of antitumor acridine agent C-1748 The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7 (2018), Pharmacol. Rep., 70, 972-980 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 C-1748 mixed-type inhibition of isoform UGT1A9 Homo sapiens

Localization

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

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens O60656
-
-
2.4.1.17 Homo sapiens O75795
-
-
2.4.1.17 Homo sapiens P16662
-
-
2.4.1.17 Homo sapiens P22309
-
-
2.4.1.17 Homo sapiens P22310
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 HT-29 cell
-
 Homo sapiens
-
2.4.1.17 intestine
-
 Homo sapiens
-
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 7-ethyl-10-hydroxy-camptothecin + UDP-glucuronate i.e SN-38, substrate for isoform UGT1A1 Homo sapiens UDP + 7-ethyl-10-hydroxy-camptothecin beta-D-glucuronide
-
 ?
2.4.1.17 7-hydroxy-4-trifluoromethylcoumarin + UDP-glucuronate
-
 Homo sapiens UDP + 7-hydroxy-4-trifluoromethylcoumarin beta-D-glucuronide
-
 ?
2.4.1.17 C-1748 + UDP-glucuronate C-1748 is 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine. The reaction is selectively catalyzed by isoform UGT2B17 Homo sapiens UDP + C-1748 O-glucuronide
-
 ?
2.4.1.17 C-1748 + UDP-glucuronate C-1748 is 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine. The reaction is selectively catalyzed by isoform UGT2B7 Homo sapiens UDP + C-1748 O-glucuronide
-
 ?
2.4.1.17 epirubicin + UDP-glucuronate substrate for isoform UGT2B7 Homo sapiens UDP + epirubicin beta-D-glucuronoside
-
 ?
2.4.1.17 trifluoperazine dihydrochloride + UDP-glucuronate substrate for isoform UGT1A4 Homo sapiens UDP + ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase
-
 Homo sapiens
2.4.1.17 UGT1A1 isoform Homo sapiens
2.4.1.17 UGT1A4 isoform Homo sapiens
2.4.1.17 UGT1A9 isoform Homo sapiens
2.4.1.17 UGT2B17 isoform Homo sapiens
2.4.1.17 UGT2B7 isoform Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.081
-
 C-1748 isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
2.4.1.17 0.0946
-
 C-1748 enzyme from HT-29 cells, at pH 7.4 and 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 0.0397
-
 isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens C-1748
2.4.1.17 0.0845
-
 enzyme from HT-29 cells, at pH 7.4 and 37°C Homo sapiens C-1748