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Literature summary for 1.5.1.3 extracted from
- Characterization of Plasmodium knowlesi dihydrofolate reductase-thymidylate synthase and sensitivity to antifolates (2018), Parasitol. Int., 67, 787-792 .
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | amplification of a DHFR gene from field isolate PKNY146CSP collected from Southern Thailand. Aanalysis shows 11 polymorphisms in the DHFR domain of the bifunctional DHFR-TS gene. One polymorphism is a non-synonymous substitution (R34L) that has been reported but not associated with antifolate resistance | Plasmodium knowlesi |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3-(2-(3-[(2,4-diamino-6-ethylpyrimidin-5-yl)oxy]propoxy)phenyl)propanoic acid | i.e. P218, a registered candidate drug in human clinical trial | Plasmodium knowlesi | |
| cycloguanil | - |
Plasmodium knowlesi |  |
| pyrimethamine | - |
Plasmodium knowlesi | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00022 | - |
7,8-dihydrofolate | pH 6, temperature not specified in the publication, isolate PKNY146CSP | Plasmodium knowlesi | |
| 0.0023 | - |
NADPH | pH 6, temperature not specified in the publication, isolate PKNY146CSP | Plasmodium knowlesi | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 147000 | - |
gel filtration | Plasmodium knowlesi |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Plasmodium knowlesi | A0A384KN43 | bifunctional dihydrofolate reductase-thymidylate synthase, cf. EC 2.1.1.45 | - |
| Plasmodium knowlesi H | A0A384KN43 | bifunctional dihydrofolate reductase-thymidylate synthase, cf. EC 2.1.1.45 | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 7,8-dihydrofolate + NADPH + H+ | - |
Plasmodium knowlesi | 5,6,7,8-tetrahydrofolate + NADP+ | - |
? | |
| 7,8-dihydrofolate + NADPH + H+ | - |
Plasmodium knowlesi H | 5,6,7,8-tetrahydrofolate + NADP+ | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| dimer | 2 * 66000, SDS-PAGE | Plasmodium knowlesi |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PKNH_0509600 | - |
Plasmodium knowlesi |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 15.9 | - |
7,8-dihydrofolate | pH 6, temperature not specified in the publication, isolate PKNY146CSP | Plasmodium knowlesi | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 6 | - |
- |
Plasmodium knowlesi |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00000003 | - |
3-(2-(3-[(2,4-diamino-6-ethylpyrimidin-5-yl)oxy]propoxy)phenyl)propanoic acid | pH 6, temperature not specified in the publication, isolate PKNY146CSP | Plasmodium knowlesi | |
| 0.00000005 | - |
pyrimethamine | pH 6, temperature not specified in the publication, isolate PKNY146CSP | Plasmodium knowlesi | |
| 0.00000011 | - |
cycloguanil | pH 6, temperature not specified in the publication, isolate PKNY146CSP | Plasmodium knowlesi | |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 6900 | - |
NADPH | pH 6, temperature not specified in the publication, isolate PKNY146CSP | Plasmodium knowlesi | |
| 72300 | - |
7,8-dihydrofolate | pH 6, temperature not specified in the publication, isolate PKNY146CSP | Plasmodium knowlesi | |
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