Application | Comment | Organism |
---|---|---|
medicine | enzyme is a target of several anti-folate inhibitory drugs to combat bacteria, protozoa and cancer | Plasmodium vivax |
Cloned (Comment) | Organism |
---|---|
DNA-sequence analysis | Plasmodium vivax |
expression in Escherichia coli of wild-type and mutant enzymes | Plasmodium vivax |
Protein Variants | Comment | Organism |
---|---|---|
S58R/S117N | double mutant with naturally occurring point mutations, antifolate drug resistant | Plasmodium vivax |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
cycloguanil | wild-type and mutant | Plasmodium vivax | |
methotrexate | wild-type and mutant | Plasmodium vivax | |
pyrimethamine | wild-type and mutant | Plasmodium vivax | |
trimethoprim | wild-type and mutant | Plasmodium vivax |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.06 | - |
NADPH | wild-type enzyme | Plasmodium vivax | |
0.07 | - |
NADPH | mutant enzyme | Plasmodium vivax | |
0.097 | - |
7,8-dihydrofolate | mutant enzyme | Plasmodium vivax | |
0.107 | - |
7,8-dihydrofolate | wild-type enzyme | Plasmodium vivax |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
7,8-dihydrofolate + NADPH | Plasmodium vivax | DHFR activity is not essential for virus replication | 5,6,7,8-tetrahydrofolate + NADP+ | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Plasmodium vivax | - |
wild-type and mutant enzymes recombinant from Escherichia coli | - |
Purification (Comment) | Organism |
---|---|
recombinant from Escherichia coli | Plasmodium vivax |
Renatured (Comment) | Organism |
---|---|
wild-type and mutant, renaturation from inclusion bodies due to expression in E. coli, 200 mM KCl, 20 mM potassium phosphate, pH 7.0, 0.1 mM EDTA, 10 mM dithiothreitol | Plasmodium vivax |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
1.7 | - |
purified recombinant enzyme | Plasmodium vivax |
Storage Stability | Organism |
---|---|
-20°C, several months | Plasmodium vivax |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
7,8-dihydrofolate + NADPH | - |
Plasmodium vivax | 5,6,7,8-tetrahydrofolate + NADP+ | - |
? | |
7,8-dihydrofolate + NADPH | DHFR activity is not essential for virus replication | Plasmodium vivax | 5,6,7,8-tetrahydrofolate + NADP+ | - |
? |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Plasmodium vivax |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Plasmodium vivax |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000052 | - |
methotrexate | wild-type enzyme | Plasmodium vivax | |
0.0000069 | - |
methotrexate | mutant enzyme | Plasmodium vivax | |
0.000064 | - |
pyrimethamine | wild-type enzyme | Plasmodium vivax | |
0.000067 | - |
cycloguanil | wild-type enzyme | Plasmodium vivax | |
0.000098 | - |
trimethoprim | wild-type enzyme | Plasmodium vivax | |
0.000143 | - |
trimethoprim | mutant enzyme | Plasmodium vivax | |
0.000743 | - |
cycloguanil | mutant enzyme | Plasmodium vivax | |
0.00093 | - |
pyrimethamine | mutant enzyme | Plasmodium vivax |