Literature summary for 6.3.2.17 extracted from

Leil, T.A.; Endo, C.; Adjei, A.A.; Dy, G.K.; Salavaggione, O.E.; Reid, J.R.; Ames, M.M.; Adjei, A.A.
Identification and characterization of genetic variation in the folylpolyglutamate synthase gene (2007), Cancer Res., 67, 8772-8782.

Search for more literature for 6.3.2.17

Cloned(Commentary)

Cloned (Comment)	Organism
expressed in AuxB1 cells	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
A447V	does not affect enzyme activity	Homo sapiens
R424C	reduced efficacy with substrates compared to the wild type enzyme	Homo sapiens
S457F	reduced efficacy with substrates compared to the wild type enzyme	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
methotrexate	-	Homo sapiens
pemetrexed	-	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.0526	-	methotrexate	wild type enzyme from mitochondrion	Homo sapiens
0.0555	-	methotrexate	wild type enzyme from cytosol	Homo sapiens
0.0613	-	methotrexate	mutant enzyme S457F	Homo sapiens
0.0827	-	methotrexate	mutant enzyme A447V	Homo sapiens
0.0908	-	methotrexate	mutant enzyme R424C	Homo sapiens
1.63	-	Glu	mutant enzyme A447V	Homo sapiens
1.702	-	Glu	wild type enzyme from cytosol	Homo sapiens
2.068	-	Glu	wild type enzyme from mitochondrion	Homo sapiens
2.281	-	Glu	mutant enzyme S457F	Homo sapiens
5.984	-	Glu	mutant enzyme R424C	Homo sapiens

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
cytosol	-	Homo sapiens	5829	-
mitochondrion	-	Homo sapiens	5739	-

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + methotrexate + Glu	-	Homo sapiens	ADP + phosphate + methotrexyl-Glu	-	?
ATP + pemetrexed + Glu	-	Homo sapiens	ADP + phosphate + pemetrexyl-Glu	-	?

Synonyms

Synonyms	Comment	Organism
Folylpolyglutamate synthase	-	Homo sapiens
FPGS	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000095	-	wild type enzyme from cytosol	Homo sapiens	methotrexate
0.000011	-	wild type enzyme from mitochondrion	Homo sapiens	pemetrexed
0.0000127	-	mutant enzyme A447V	Homo sapiens	pemetrexed
0.0000129	-	mutant enzyme A447V	Homo sapiens	methotrexate
0.0000136	-	wild type enzyme from cytosol	Homo sapiens	pemetrexed
0.0000145	-	wild type enzyme from mitochondrion	Homo sapiens	methotrexate
0.0000156	-	mutant enzyme S457F	Homo sapiens	methotrexate
0.0000175	-	mutant enzyme R424C	Homo sapiens	methotrexate
0.0000263	-	mutant enzyme R424C	Homo sapiens	pemetrexed
0.0000302	-	mutant enzyme S457F	Homo sapiens	pemetrexed

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Release 2023.1 (January 2023)