Literature summary for 2.4.1.17 extracted from

Fedejko-Kap, B.; Bratton, S.M.; Finel, M.; Radominska-Pandya, A.; Mazerska, Z.
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10 (2012), Drug Metab. Dispos., 40, 1736-1743.

Search for more literature for 2.4.1.17

Application

Application	Comment	Organism
medicine	imidazoacridinone and triazoloacridinone drugs are glucuronidated in human liver	Homo sapiens

Cloned(Commentary)

Cloned (Comment)	Organism
expression in insect cell	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
D396A	mutation in isoform UGT1A10, activity toward substrates 5-diethylaminoethylamino-8-hydroxyimidazoacridinone and 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone is decreased by 30% and increased by 25%, respectively	Homo sapiens
V92A	mutation in isoform UGT1A10, activity toward substrates 5-diethylaminoethylamino-8-hydroxyimidazoacridinone and 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone is decreased by 60% and 72%, respectively, accompanied by increase in affinity to these substrates	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
5-diethylaminoethylamino-8-hydroxyimidazoacridinone	substrate inhibition with isoform UGT1A9	Homo sapiens
5-dimethylaminopropylamino-8-hydroxytriazoloacridinone	substrate inhibition with isoform UGT1A9	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.0289	-	5-dimethylaminopropylamino-8-hydroxytriazoloacridinone	isoform UGT1A1, pH not specified in the publication, temperature not specified in the publication	Homo sapiens
0.0293	-	5-diethylaminoethylamino-8-hydroxyimidazoacridinone	isoform UGT1A7, pH not specified in the publication, temperature not specified in the publication	Homo sapiens
0.0546	-	5-diethylaminoethylamino-8-hydroxyimidazoacridinone	isoform UGT1A9, pH not specified in the publication, temperature not specified in the publication	Homo sapiens
0.0633	-	5-dimethylaminopropylamino-8-hydroxytriazoloacridinone	isoform UGT1A9, pH not specified in the publication, temperature not specified in the publication	Homo sapiens
0.0706	-	5-dimethylaminopropylamino-8-hydroxytriazoloacridinone	isoform UGT1A10, pH not specified in the publication, temperature not specified in the publication	Homo sapiens
0.094	-	5-diethylaminoethylamino-8-hydroxyimidazoacridinone	isoform UGT1A10, pH not specified in the publication, temperature not specified in the publication	Homo sapiens
0.149	-	5-diethylaminoethylamino-8-hydroxyimidazoacridinone	isoform UGT1A1, pH not specified in the publication, temperature not specified in the publication	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
liver	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
5-diethylaminoethylamino-8-hydroxyimidazoacridinone + UDP-alpha-D-glucuronate	i.e. antitumor agent C-1311, NSC-645809	Homo sapiens	5-{[2-(diethylamino)ethyl]amino}-6-oxo-6H-imidazo[4,5,1-de]acridin-8-yl beta-D-glucuronide + UDP	-	?
5-dimethylaminopropylamino-8-hydroxytriazoloacridinone + UDP-alpha-D-glucuronate	i.e. antitumor agent C-1305	Homo sapiens	5-dimethylaminopropylamino-8-hydroxytriazoloacridinone-8-D-glucuronide + UDP	-	?

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.958	-	5-dimethylaminopropylamino-8-hydroxytriazoloacridinone	isoform UGT1A9, pH not specified in the publication, temperature not specified in the publication	Homo sapiens
1.651	-	5-diethylaminoethylamino-8-hydroxyimidazoacridinone	isoform UGT1A9, pH not specified in the publication, temperature not specified in the publication	Homo sapiens

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Release 2023.1 (January 2023)