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Literature summary for 2.7.4.8 extracted from
- 9-(Phosphonoalkyl)guanine derivatives as substrates or inhibitors of guanylate kinase (1992), Arch. Biochem. Biophys., 295, 253-257.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 9-(6,6-difluoro-6-phosphonohexyl)guanine | competitive with respect to GMP, non-competitive with respect to ATP | Sus scrofa |  |
| 9-(6-phosphonohexyl)guanine | competitive with respect to GMP, non-competitive with respect to ATP | Sus scrofa | |
| additional information | no inhibition by 9-(5-phosphonopentyl)guanine (i.e. isosteric analogue of acyclovir 5'-monophosphate) | Sus scrofa |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.032 | - |
GMP | pH 7.5, 30ºC | Sus scrofa | |
| 0.083 | - |
dGMP | pH 7.5, 30ºC | Sus scrofa | |
| 0.25 | - |
9-(5-phosphonopentyl)guanine | pH 7.5, 30ºC | Sus scrofa | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Sus scrofa | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + GMP | Sus scrofa | key enzyme of biosynthetic pathway of GTP or dGTP | ADP + GDP | - |
r | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Sus scrofa | - |
pig | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Sus scrofa | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + 9-(1,3-dihydroxy-2-propoxymethyl)guanine 5'-monophosphate | no substrate: 9-(5,5-difluoro-5-phosphonopentyl)guanine 5'-monophosphate | Sus scrofa | ADP + 9-(1,3-dihydroxy-2-propoxymethyl)guanine 5'-diphosphate | - |
? | |
| ATP + 9-(2-hydroxyethoxymethyl)guanine 5'-monophosphate | i.e. acyclovir 5'-monophosphate | Sus scrofa | ADP + 9-(2-hydroxyethoxymethyl)guanine 5'-diphosphate | - |
? | |
| ATP + 9-(5-phosphonopentyl)guanine | 9-(5,5'-difluoro-5-phosphonopenthyl)guanine is not a substrate | Sus scrofa | ? | - |
? | |
| ATP + dGMP | - |
Sus scrofa | ADP + dGDP | - |
r | |
| ATP + GMP | - |
Sus scrofa | ADP + GDP | - |
? | |
| ATP + GMP | key enzyme of biosynthetic pathway of GTP or dGTP | Sus scrofa | ADP + GDP | - |
r | |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Sus scrofa |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Sus scrofa |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.11 | - |
9-(6-phosphonohexyl)guanine | pH 7.5, 30ºC | Sus scrofa | |
| 0.14 | - |
9-(6,6-difluoro-6-phosphonohexyl)guanine | pH 7.5, 30ºC, higher affinity than 9-(6-phosphonohexyl)guanine for guanylate kinases al pH values below 7.5 | Sus scrofa | |
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