Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.1.1.45 extracted from

  • Gangjee, A.; Jain, H.D.; Phan, J.; Guo, X.; Queener, S.F.; Kisliuk, R.L.
    2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors (2010), Bioorg. Med. Chem., 18, 953-961.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
methotrexate
-
Escherichia coli
methotrexate
-
Homo sapiens
methotrexate
-
Toxoplasma gondii
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
Escherichia coli
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
Homo sapiens
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
Toxoplasma gondii
pemetrexed
-
Escherichia coli
pemetrexed
-
Homo sapiens
pemetrexed
-
Toxoplasma gondii
raltitrexed
-
Escherichia coli
raltitrexed
-
Homo sapiens
raltitrexed
-
Toxoplasma gondii
trimethoprim
-
Escherichia coli
trimethoprim
-
Homo sapiens
trimethoprim
-
Toxoplasma gondii
trimetrexate
-
Escherichia coli
trimetrexate
-
Homo sapiens
trimetrexate
-
Toxoplasma gondii

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Homo sapiens
-
-
-
Toxoplasma gondii
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,10-methylenetetrahydrofolate + dUMP
-
Escherichia coli dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP
-
Homo sapiens dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP
-
Toxoplasma gondii dihydrofolate + dTMP
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00038
-
at 30°C and pH 7.4 Homo sapiens raltitrexed
0.0009
-
at 30°C and pH 7.4 Toxoplasma gondii raltitrexed
0.0028
-
at 30°C and pH 7.4 Toxoplasma gondii pemetrexed
0.0054
-
at 30°C and pH 7.4 Homo sapiens N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
0.0057
-
at 30°C and pH 7.4 Escherichia coli raltitrexed
0.0095
-
at 30°C and pH 7.4 Homo sapiens pemetrexed
0.018
-
at 30°C and pH 7.4 Toxoplasma gondii methotrexate
0.027
-
at 30°C and pH 7.4 Toxoplasma gondii N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
0.029
-
at 30°C and pH 7.4 Homo sapiens methotrexate
0.076
-
at 30°C and pH 7.4 Escherichia coli pemetrexed
0.09
-
at 30°C and pH 7.4 Escherichia coli methotrexate
0.23
-
at 30°C and pH 7.4 Escherichia coli N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid