Cloned (Comment) | Organism |
---|---|
gene PVX_092040 | Plasmodium vivax |
Crystallization (Comment) | Organism |
---|---|
purified recombinant GGPPS, in apo form or in complex with zoledronate, hanging drop vapour diffusion method, for the apo enzyme crystals: 0.0015 ml of 16.5 mg/ml protein in 10 mM HEPES, pH 7.5, 500 mM NaCl, is mixed with 0.0015 ml of reservoir solution containing 22% PEG 3350, 200 mM Li2SO4, 100 mM Tris, pH 8.5, for the inhibitor complex crystals: 0.0015 ml of 11.2 mg/ml protein and 10 mM zoledronate, 10 mM IPP, 10 mM MgCl2, 10 mM HEPES, pH 7.5, 500 mM NaCl are mixed with 0.0015 ml reservoir solution containing 20% PEG 3350, 200 mM Li2SO4, 100 mM Tris, 8.5, 18°C, overnight, X-ray diffraction structure determination and analysis at 2.1 A resolution | Plasmodium vivax |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
ibandronate | a nitrogen-containing bisphosphonate | Plasmodium vivax | |
nitrogen-containing bisphosphonates | Plasmodium vivax GGPP synthase can bind nitrogen-containing bisphosphonates strongly with the energetically favorable cooperation of three Mg2+, resulting in inhibition at IC50 concentrations below 100 nM. The aspartates at the start and end of the five-residue motif, the second aspartate-rich motif, in Plasmodium vivax GGPPSs both participate in the coordination of the third Mg2+ | Plasmodium vivax | |
zoledronate | a nitrogen-containing bisphosphonate | Plasmodium vivax | |
[1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid | a nitrogen-containing bisphosphonate | Plasmodium vivax |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0019 | - |
geranyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
0.0032 | - |
dimethylallyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
0.0073 | - |
(2E,6E)-farnesyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
0.0084 | - |
isopentenyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Plasmodium vivax |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
(2E,6E)-farnesyl diphosphate + isopentenyl diphosphate | Plasmodium vivax | - |
diphosphate + geranylgeranyl diphosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Plasmodium vivax | - |
gene PVX_092040 | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
(2E,6E)-farnesyl diphosphate + isopentenyl diphosphate | - |
Plasmodium vivax | diphosphate + geranylgeranyl diphosphate | - |
? | |
geranyl diphosphate + dimethylallyl diphosphate | - |
Plasmodium vivax | diphosphate + geranylgeranyl diphosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
geranylgeranyl pyrophosphate synthase | - |
Plasmodium vivax |
GGPP synthase | - |
Plasmodium vivax |
GGPPS | - |
Plasmodium vivax |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Plasmodium vivax |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.5 | - |
dimethylallyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
0.5 | - |
geranyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
0.8 | - |
(2E,6E)-farnesyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
0.8 | - |
isopentenyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.7 | - |
assay at | Plasmodium vivax |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000107 | - |
zoledronate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
0.0000124 | - |
[1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
0.000016 | - |
ibandronate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000433 | - |
pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | zoledronate | |
0.0000475 | - |
pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | [1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid | |
0.0000619 | - |
pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | ibandronate |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
100 | - |
(2E,6E)-farnesyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
200 | - |
dimethylallyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax | |
300 | - |
geranyl diphosphate | pH 7.7, 37°C, recombinant PvGGPPS | Plasmodium vivax |