Cloned (Comment) | Organism |
---|---|
expression in Sf9 cells with recombinant baculovirus | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid | 3-PEHPC, weak inhibitor, 100% activity remain with concentrations up to 1 microM inhibitor and substrate Rab1a, with 10 microM inhibitor about 60% activity remain, with 100 microM and more inhibitor the activity falls to 30% and below | Homo sapiens | |
2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid | (+)-3-IPEHPC, the (+)-enantiomer is selective towards the enzyme and more potent than the (-)-enantiomer, mixed type inhibitor with respect to geranylgeranyl diphosphate, uncompetitive inhibitor with respect to Rab substrate, 25fold more potent than 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid, with 1 microM inhibitor activity falls to about 50%, with 10 microM inhibitor and more activity falls below 20% | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
geranylgeranyl diphosphate + Rab | Homo sapiens | His6- and gluthathione S-transferase-tagged Rab proteins such as canine Rab1a, human Rab27a, Rab5a, Rab18, Rab6a, Rab13, and mouse Rab23 | S-geranylgeranyl-Rab + diphosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
nickel-Sepharose affinity chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
geranylgeranyl diphosphate + Rab | His6- and gluthathione S-transferase-tagged Rab proteins such as canine Rab1a, human Rab27a, Rab5a, Rab18, Rab6a, Rab13, and mouse Rab23 | Homo sapiens | S-geranylgeranyl-Rab + diphosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Rab geranylgeranyltransferase type II | - |
Homo sapiens |
RGGT | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.005 | - |
2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid | mixed-type inhibition with geranylgeranyl diphosphate 1 as variable substrate, 50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 4 microM Rab1a, 50 nM enzyme, 20 min, 37°C | Homo sapiens | |
0.03356 | - |
2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid | uncompetitive reaction with Rab1a as variable substrate, 50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 5 microM geranylgeranyl diphosphate 1, 50 nM enzyme, 20 min, 37°C | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
additional information | - |
the inhibitory action of 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid with substrates Rab1a-CSC and Rab1a-CCS are not determined, and is not significant (IC50 > 2 mM) with the substrates Rab1a-CS, Rab1aSC, Rab27a-CVLS, Rab5a-CCQNI, Rab5a-CVLL, Rab13-CSLG (wild type), Rab18-CSVL (wild type), and Rab23-CSVP (wild type), and IC50 > 1.592 mM with Rab6a-CSC | Homo sapiens | additional information | |
0.03185 | - |
50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 6 microM tritium-labelled geranylgeranyl diphosphate, 4 microM Rab1a-CC (wild type), 2 microM Rab escort protein 1, 50 nM enzyme, 20 min, 37°C | Homo sapiens | 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid | |
0.03268 | - |
50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 6 microM tritium-labelled geranylgeranyl diphosphate, 4 microM Rab27a-CGC (wild type), 2 microM Rab escort protein 1, 50 nM enzyme, 20 min, 37°C | Homo sapiens | 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid | |
0.04347 | - |
50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 6 microM tritium-labelled geranylgeranyl diphosphate, 4 microM Rab5a-CCSN (wild type), 2 microM Rab escort protein 1, 50 nM enzyme, 20 min, 37°C | Homo sapiens | 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid | |
0.86 | - |
50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 6 microM tritium-labelled geranylgeranyl diphosphate, 4 microM Rab5a-CCVLL, 2 microM Rab escort protein 1, 50 nM enzyme, 20 min, 37°C | Homo sapiens | 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid |