Application | Comment | Organism |
---|---|---|
drug development | the enzyme represents an attractive target for inhibitor design to disrupt systems that require rapid DNA turnover, e.g. proliferating cancer cells and pathogenic microbes | Escherichia coli |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(4-nitrophenyl)-3-[4-[4-[(4-nitrophenyl)carbamoylamino]phenoxy]phenyl]urea | NSC80735, complete inhibition at 1 mM | Escherichia coli | |
1-N,4-N-bis(4-aminophenyl)benzene-1,4-dicarboxamide | NSC55152, complete inhibition at 1 mM | Escherichia coli | |
11H-benzo[b][1]benzazepine | NSC123458, 87% inhibition at 1 mM | Escherichia coli | |
6,7-bis(4-aminophenyl)pteridine-2,4-diamine | NSC61642 | Escherichia coli | |
7-[(4-aminophenyl)methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine | NSC309401, AMPQD, a substrate analogue with the quinazoline-1, 3-diamine group, tight-binding inhibitor, complete inhibition at 1 mM, competitive inhibition of dihydrofolate binding. Potently inhibits the enzyme by competitive displacement of the substrate dihydrofolic acid, uncompetitive inhibition versus NADPH, the inhibitor has a markedly increased affinity for the NADPH-bound form of the enzyme. The mode of binding of the inhibitor to the enzyme-NADPH binary complex conforms to the slow-onset, tight-binding model | Escherichia coli | |
7H-pyrrolo(3,2-f)quinazoline-1,3-diamine | NSC339578 | Escherichia coli | |
7H-pyrrolo[3,2-f]quinazoline-1,3-diamine | PQD, the lack of (4-aminophenyl)-methyl group at position 7 abolishes the slow-onset of inhibition | Escherichia coli | |
methotrexate | NSC740 | Escherichia coli | |
methylbenzoprim | NSC382035 | Escherichia coli | |
additional information | 7H-pyrrolo(3,2-f) quinazoline-1, 3-diamine (PQD) inhibition kinetics, overview | Escherichia coli | |
pemetrexed | NSC698037 | Escherichia coli | |
pralatrexate | NSC754230 | Escherichia coli |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten kinetics | Escherichia coli |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
7,8-dihydrofolate + NADPH + H+ | Escherichia coli | - |
5,6,7,8-tetrahydrofolate + NADP+ | - |
r |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Escherichia coli | P0ABQ4 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
7,8-dihydrofolate + NADPH + H+ | - |
Escherichia coli | 5,6,7,8-tetrahydrofolate + NADP+ | - |
r |
Synonyms | Comment | Organism |
---|---|---|
DHFR | - |
Escherichia coli |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADP+ | - |
Escherichia coli | |
NADPH | - |
Escherichia coli |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics, overview | Escherichia coli | |
0.00000742 | - |
7-[(4-aminophenyl)methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine | pH 7.3, 22°C | Escherichia coli |