Literature summary for 2.4.1.17 extracted from

Zhang, D.; Chando, T.J.; Everett, D.W.; Patten, C.J.; Dehal, S.S.; Humphreys, W.G.
In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation (2005), Drug Metab. Dispos., 33, 1729-1739.

Search for more literature for 2.4.1.17

Inhibitors

Inhibitors	Comment	Organism	Structure
2-hydroxy-estradiol	38.5% inhibition at 0.1 mM, UGT1A3	Homo sapiens
atazanavir	a HIV protease inhibitor, linear mixed-type inhibition mechanism, UGT1A1, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7	Homo sapiens
beta-estradiol	61.5% inhibition at 0.2 mM, UGT1A1	Homo sapiens
eugenol	UGT2B7, 54.5% inhibition at 0.1 mM	Homo sapiens
hecogenin	48.0% inhibition at 0.05 mM, UGT1A4	Homo sapiens
indinavir	a HIV protease inhibitor, linear mixed-type inhibition mechanism, UGT1A1, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7	Homo sapiens
lopinavir	a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7	Homo sapiens
additional information	IC50 values for HIV protease inhibitors with UGT isozymes, overview	Homo sapiens
naphthol	UGT1A6, 87.0% inhibition at 0.05 mM	Homo sapiens
nelfinavir	a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7	Homo sapiens
propofol	UGT1A9, 37.0% inhibition at 0.05 mM	Homo sapiens
ritonavir	a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7	Homo sapiens
saquinavir	a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.004	-	bilirubin	pH 7.5, 37°C, recombinant UGT1A1	Homo sapiens
0.0062	-	bilirubin	pH 7.5, 37°C, liver UGT1A1	Homo sapiens

Localization

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

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	-	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
additional information	Homo sapiens	direct inhibition of UGT1A1-mediated bilirubin glucuronidation may provide a mechanism for the reversible hyperbilirubinemia associated with administration of atazanavir as well as indinavir	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	isozymes UGT1A1, 1A3, 1A4, 1A6, 1A9, and 2B7	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
commercial preparation	human UGT supersomes, i.e. membranes of insect cells transfected with baculovirus containing human cDNA of UGTs or microsomes of lymphoblast cells heterologously expressing human cDNA of UGT1A1	Homo sapiens	-
liver	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	direct inhibition of UGT1A1-mediated bilirubin glucuronidation may provide a mechanism for the reversible hyperbilirubinemia associated with administration of atazanavir as well as indinavir	Homo sapiens	?	-	?
UDP-glucuronic acid + 7-hydroxy-4-(trifluoromethyl)-coumarin	UGT1A6, UGT1A9, and UGT2B7	Homo sapiens	UDP + 7-hydroxy-4-(trifluoromethyl)-coumarin O-glucuronide	-	?
UDP-glucuronic acid + beta-estradiol	UGT1A3	Homo sapiens	UDP + beta-estradiol 3-O-beta-D-glucuronide	-	?
UDP-glucuronic acid + bilirubin	UGT1A1	Homo sapiens	UDP + bilirubin-glucuronoside	-	?
UDP-glucuronic acid + trifluoperazine	UGT1A4	Homo sapiens	UDP + ?	-	?

Synonyms

Synonyms	Comment	Organism
UGT	-	Homo sapiens
uridine 5'-diphospho-glucuronosyltransferase	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at, UGT1A1	Homo sapiens

pH Optimum

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

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
additional information	-	additional information	inhibition kinetics	Homo sapiens
0.0019	-	atazanavir	pH 7.5, 37°C, UGT1A1	Homo sapiens
0.0479	-	indinavir	pH 7.5, 37°C, UGT1A1	Homo sapiens

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Release 2023.1 (January 2023)