Cloned (Comment) | Organism |
---|---|
expression in Escherichia coli | Plasmodium falciparum |
Protein Variants | Comment | Organism |
---|---|---|
I51N/C59R/N108S/I164L | mutant isolated in an effort to mimic the impact of drug pressure on the selection of dihydrofolate reductase mutations in the malaria parasite population, based on DHFR-TS-QM mutation which exhibits the highest degree of antifolate resistance developed in the field | Plasmodium falciparum |
N51I/C59R/N108S/I164L | mutant isolated in an effort to mimic the impact of drug pressure on the selection of dihydrofolate reductase mutations in the malaria parasite population, based on DHFR-TS-QM mutation which exhibits the highest degree of antifolate resistance developed in the field | Plasmodium falciparum |
N51I/C59R/N108T/I164L | mutant isolated in an effort to mimic the impact of drug pressure on the selection of dihydrofolate reductase mutations in the malaria parasite population, based on DHFR-TS-QM mutation which exhibits the highest degree of antifolate resistance developed in the field | Plasmodium falciparum |
N51I/C59R/S108N/I164L | mutant highly resistant to pyrimethamine, but sensitive to WR99210, i.e. DHFT-QM mutant | Plasmodium falciparum |
N51I/C59R/S108N/I164L/D187A | mutant isolated in an effort to mimic the impact of drug pressure on the selection of dihydrofolate reductase mutations in the malaria parasite population, based on DHFR-TS-QM mutation which exhibits the highest degree of antifolate resistance developed in the field | Plasmodium falciparum |
N51I/C59R/S108N/I164L/I150V/N182I/N201D | mutant isolated in an effort to mimic the impact of drug pressure on the selection of dihydrofolate reductase mutations in the malaria parasite population, based on DHFR-TS-QM mutation which exhibits the highest degree of antifolate resistance developed in the field | Plasmodium falciparum |
N51I/C59R/S108N/I164L/K96N | mutant isolated in an effort to mimic the impact of drug pressure on the selection of dihydrofolate reductase mutations in the malaria parasite population, based on DHFR-TS-QM mutation which exhibits the highest degree of antifolate resistance developed in the field | Plasmodium falciparum |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
pyrimethamine | - |
Plasmodium falciparum | |
WR99210 | - |
Plasmodium falciparum |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.005 | - |
7,8-dihydrofolate | mutant N51I/C59R/N108T/I164L, pH 7.0 | Plasmodium falciparum | |
0.0052 | - |
7,8-dihydrofolate | mutant N51I/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
0.00595 | - |
NADPH | mutant N51I/C59R/N108T/I164L, pH 7.0 | Plasmodium falciparum | |
0.00643 | - |
NADPH | mutant N51I/C59R/S108N/I164L, pH 7.0 | Plasmodium falciparum | |
0.0065 | - |
NADPH | mutant N51I/C59R/S108N/I164L/D187A, pH 7.0 | Plasmodium falciparum | |
0.0072 | - |
NADPH | mutant N51I/C59R/S108N/I164L/K96N, pH 7.0 | Plasmodium falciparum | |
0.0081 | - |
7,8-dihydrofolate | mutant N51I/C59R/S108N/I164L/K96N, pH 7.0 | Plasmodium falciparum | |
0.0083 | - |
7,8-dihydrofolate | mutant I51N/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
0.0113 | - |
NADPH | mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0 | Plasmodium falciparum | |
0.0133 | - |
7,8-dihydrofolate | mutant N51I/C59R/S108N/I164L, pH 7.0 | Plasmodium falciparum | |
0.0145 | - |
7,8-dihydrofolate | mutant N51I/C59R/S108N/I164L/D187A, pH 7.0 | Plasmodium falciparum | |
0.01465 | - |
7,8-dihydrofolate | mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0 | Plasmodium falciparum | |
0.0267 | - |
NADPH | mutant I51N/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
0.052 | - |
NADPH | mutant N51I/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Plasmodium falciparum | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
7,8-dihydrofolate + NADPH + H+ | - |
Plasmodium falciparum | 5,6,7,8-tetrahydrofolate + NADP+ | - |
? |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.2 | - |
7,8-dihydrofolate | mutant I51N/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
1.5 | - |
7,8-dihydrofolate | mutant N51I/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
1.9 | - |
7,8-dihydrofolate | mutant N51I/C59R/N108T/I164L, pH 7.0 | Plasmodium falciparum | |
11.4 | - |
7,8-dihydrofolate | mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0 | Plasmodium falciparum | |
13.6 | - |
7,8-dihydrofolate | mutant N51I/C59R/S108N/I164L/D187A, pH 7.0 | Plasmodium falciparum | |
28.3 | - |
7,8-dihydrofolate | mutant N51I/C59R/S108N/I164L/K96N, pH 7.0 | Plasmodium falciparum | |
72 | - |
7,8-dihydrofolate | mutant N51I/C59R/S108N/I164L, pH 7.0 | Plasmodium falciparum |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00000085 | - |
WR99210 | mutant N51I/C59R/S108N/I164L/K96N, pH 7.0 | Plasmodium falciparum | |
0.0000011 | - |
WR99210 | mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0 | Plasmodium falciparum | |
0.0000012 | - |
WR99210 | mutant N51I/C59R/S108N/I164L/D187A, pH 7.0 | Plasmodium falciparum | |
0.0000021 | - |
WR99210 | mutant N51I/C59R/S108N/I164L, pH 7.0 | Plasmodium falciparum | |
0.0000036 | - |
WR99210 | mutant I51N/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
0.0000073 | - |
WR99210 | mutant N51I/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
0.0000081 | - |
pyrimethamine | mutant I51N/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
0.0000155 | - |
WR99210 | mutant N51I/C59R/N108T/I164L, pH 7.0 | Plasmodium falciparum | |
0.0000176 | - |
pyrimethamine | mutant N51I/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | |
0.0000724 | - |
pyrimethamine | mutant N51I/C59R/N108T/I164L, pH 7.0 | Plasmodium falciparum | |
0.000147 | - |
pyrimethamine | mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0 | Plasmodium falciparum | |
0.000209 | - |
pyrimethamine | mutant N51I/C59R/S108N/I164L, pH 7.0 | Plasmodium falciparum | |
0.000292 | - |
pyrimethamine | mutant N51I/C59R/S108N/I164L/K96N, pH 7.0 | Plasmodium falciparum | |
0.000514 | - |
pyrimethamine | mutant N51I/C59R/S108N/I164L/D187A, pH 7.0 | Plasmodium falciparum |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00001 | - |
mutant N51I/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | pyrimethamine | |
0.00005 | - |
mutant N51I/C59R/S108N/I164L/D187A, pH 7.0 | Plasmodium falciparum | WR99210 | |
0.00006 | - |
mutant N51I/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | WR99210 | |
0.00009 | - |
mutant I51N/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | pyrimethamine | |
0.00009 | - |
mutant N51I/C59R/S108N/I164L/K96N, pH 7.0 | Plasmodium falciparum | WR99210 | |
0.00016 | - |
mutant N51I/C59R/S108N/I164L, pH 7.0 | Plasmodium falciparum | WR99210 | |
0.00017 | - |
mutant N51I/C59R/S108N/I164L, pH 7.0 | Plasmodium falciparum | pyrimethamine | |
0.0002 | - |
mutant I51N/C59R/N108S/I164L, pH 7.0 | Plasmodium falciparum | WR99210 | |
0.00068 | - |
mutant N51I/C59R/N108T/I164L, pH 7.0 | Plasmodium falciparum | WR99210 | |
0.00087 | - |
mutant N51I/C59R/S108N/I164L/D187A, pH 7.0 | Plasmodium falciparum | pyrimethamine | |
0.00092 | - |
mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0 | Plasmodium falciparum | WR99210 | |
0.00182 | - |
mutant N51I/C59R/N108T/I164L, pH 7.0 | Plasmodium falciparum | pyrimethamine | |
0.00248 | - |
mutant N51I/C59R/S108N/I164L/K96N, pH 7.0 | Plasmodium falciparum | pyrimethamine | |
0.00347 | - |
mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0 | Plasmodium falciparum | pyrimethamine |