Literature summary for 2.4.1.17 extracted from

Patana, A.; Kurkela, M.; Finel, M.; Goldman, A.
Mutation analysis in UGT1A9 suggests a relationship between substrate and catalytic residues in UDP-glucuronosyltransferases (2008), Protein Eng. Des. Sel., 21, 537-543.

Search for more literature for 2.4.1.17

Protein Variants

Protein Variants	Comment	Organism
D143A	increase in substrate inhibition with 4-methylumbelliferone, large decrease in Vmax	Homo sapiens
D148A	large decrease in Vmax	Homo sapiens
H37A	H37 is not critical in N-glucuronidation, but in O-glucuronidation. 99% decrease in Vmax with substrate UDP-glucuronate	Homo sapiens
H37D	H37 is not critical in N-glucuronidation, but in O-glucuronidation	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
4-Methylumbelliferone	substrate inhibition	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.015	-	4-Methylumbelliferone	mutant D143A	Homo sapiens
0.021	-	4-Methylumbelliferone	wild-type	Homo sapiens
0.058	-	retigabine	mutant H37A	Homo sapiens
0.062	-	scopoletin	mutant D143A	Homo sapiens
0.083	-	scopoletin	wild-type	Homo sapiens
0.09	-	retigabine	wild-type	Homo sapiens
0.138	-	UDP-glucuronate	mutant D143A	Homo sapiens
0.173	-	UDP-glucuronate	mutant H37A	Homo sapiens
0.179	-	UDP-glucuronate	wild-type	Homo sapiens
0.184	-	UDP-glucuronate	mutant D148A	Homo sapiens
0.251	-	4-aminobiphenyl	mutant D148A	Homo sapiens
0.269	-	4-aminobiphenyl	wild-type	Homo sapiens
0.286	-	4-aminobiphenyl	mutant H37A	Homo sapiens
0.629	-	scopoletin	mutant D148A	Homo sapiens
0.954	-	scopoletin	mutant H37A	Homo sapiens
0.967	-	4-Methylumbelliferone	mutant D148A	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	isoform UGT1A9	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
4-aminobiphenyl + UDP-glucuronate	-	Homo sapiens	UDP + 4-aminobiphenyl N-glucuronide	-	?
4-methylumbelliferone + UDP-glucuronate	-	Homo sapiens	UDP + 4-methylumbelliferyl-7-O-beta-D-glucuronide	-	?
retigabine + UDP-glucuronate	-	Homo sapiens	UDP + retigabine N-glucuronide	-	?
scopoletin + UDP-glucuronate	-	Homo sapiens	UDP + scopoletin O-glucuronide	-	?

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
1.2	-	4-Methylumbelliferone	mutant D143A	Homo sapiens
3.73	-	4-Methylumbelliferone	wild-type	Homo sapiens

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Release 2023.1 (January 2023)