Application | Comment | Organism |
---|---|---|
medicine | drug target | Leishmania major |
Cloned (Comment) | Organism |
---|---|
cloning of gene encoding mutant R53M enzyme from methotrexate-resistant strain into an expression plasmid, expression in Escherichia coli | Leishmania major |
Protein Variants | Comment | Organism |
---|---|---|
R53M | resistance providing naturally occurring mutant from methotrexate-resistant strain, lower turnover number | Leishmania major |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
methotrexate | wild-type enzyme, slow binding | Leishmania major | |
additional information | binding study of mutant R53M enzyme from methotrexate resistant strain with methotrexate | Leishmania major |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0009 | - |
NADPH | wild-type enzyme | Leishmania major | |
0.0012 | - |
NADPH | mutant R53M enzyme | Leishmania major | |
0.0013 | - |
7,8-dihydrofolate | wild-type enzyme | Leishmania major | |
0.0016 | - |
7,8-dihydrofolate | mutant R53M enzyme | Leishmania major |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Leishmania major | - |
bifunctional enzyme dihydrofolate reductase-thymidylate synthase | - |
Leishmania major | - |
methotrexate-resistant strain with altered enzyme | - |
Source Tissue | Comment | Organism | Textmining |
---|
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
8 | - |
wild-type enzyme | Leishmania major |
15 | - |
mutant R53M enzyme | Leishmania major |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
7,8-dihydrofolate + NADPH | - |
Leishmania major | 5,6,7,8-tetrahydrofolate + NADP+ | - |
? |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
7.6 | - |
7,8-dihydrofolate | mutant R53M enzyme | Leishmania major | |
29 | - |
7,8-dihydrofolate | wild-type enzyme | Leishmania major |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Leishmania major |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000018 | - |
methotrexate | wild-type enzyme | Leishmania major |