Application | Comment | Organism |
---|---|---|
drug development | the highly sensitive fluorescent assay for the hydrolysis of pantothenate-7-amido-4-methylcoumarin as substrate to pantothenic acid and 7-amino-4-methylcoumarin could be a powerful tool for target validation and drug lead identification and characterization | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expressed in CHO cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2,3-bis[(2-hydroxyethyl)thio]-1,4-naphthoquinone | i.e. NSC 95397, from library of pharmacologically active compounds, LOPAC | Homo sapiens | |
2-mercaptoethanol | reduced vanin-1 activity | Homo sapiens | |
5-(N,N-Hexamethylene)amiloride | from library of pharmacologically active compounds, LOPAC | Homo sapiens | |
8-cyclopentyl-1,3-dipropylxanthine | from library of pharmacologically active compounds, LOPAC | Homo sapiens | |
beta-lapachone | from library of pharmacologically active compounds, LOPAC | Homo sapiens | |
dithiothreitol | vanin-1 activity is reduced in the absence of dithiothreitol and in the presence of a high level of 50 mM dithiothreitol | Homo sapiens | |
N2-(cis-2-aminocyclohexyl)-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine hydrochloride | i.e. CGP-74514A hydrochloride, from library of pharmacologically active compounds, LOPAC | Homo sapiens | |
roscovitine | from library of pharmacologically active compounds, LOPAC | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
13 | - |
pantothenate-7-amido-4-methylcoumarin | apparent Km value, soluble recombinant vanin-1, pH 7.7, 25°C | Homo sapiens | |
28 | - |
pantothenate-7-amido-4-methylcoumarin | apparent Km value, HPLC assay, pH 7.7, 25°C | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
extracellular | the purified recombinant vanin-1 consists of a extracellular portion without a glycosylphosphatidylinositol linker | Homo sapiens | - |
- |
soluble | an highly sensitive fluorescent assay using a novel fluorescent pantotheine derivative is used for characterization of a soluble version of human vanin-1 recombinant protein, identification of hits from high-throughput screening, and quantification of vanin pantotheinase acitivity in cell lines and tissues | Homo sapiens | - |
- |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
dithiothreitol | important for vanin-1 activity, vanin-1 activity is reduced in the absence of dithiothreitol and in the presence of a high level of 50 mM dithiothreitol. Optimal concentration: 0.4 mM | Homo sapiens |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
54000 | - |
size exclusion chromatography-multiangular light scattering (SEC-MALS) | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Mus musculus | - |
C57BI/6 mice | - |
Purification (Comment) | Organism |
---|---|
recombinant enzyme,His- and Flag-tagged vanin-1 is purified over a 10 ml HisTrap Fast Flow column (a nickel affinity chromatography), 95% purity | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
kidney | higher level in kidney than in liver, determined by RT-PCR | Mus musculus | - |
liver | higher level in kidney than in liver, similar expression in lung, determined by RT-PCR | Mus musculus | - |
lung | similar expression like in liver, determined by RT-PCR | Mus musculus | - |
NCI-H292 cell | lung epithelial cells, transfected and selected for stable expression of human vanin-1 | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
pantetheine + H2O | development of a highly sensitive fluorescent assay using a novel fluorescently labeled pantotheine derivative for high throughput screening for drug development and for quantification in various cell types and tissues | Homo sapiens | pantothenic acid + cysteamine | - |
? | |
pantothenate-7-amido-4-methylcoumarin + H2O | - |
Mus musculus | pantothenic acid + 7-amino-4-methylcoumarin | based on LC-MS analysis | ? | |
pantothenate-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | pantothenic acid + 7-amino-4-methylcoumarin | based on LC-MS analysis, demonstrating that pantothenate-7-amido-4-methylcoumarin is hydrolyzed by vanin-1 at the amide-bond | ? |
Synonyms | Comment | Organism |
---|---|---|
pantetheinase | - |
Mus musculus |
pantetheinase | - |
Homo sapiens |
vanin-1 | - |
Mus musculus |
vanin-1 | belongs to the nitrilase superfamily, which contains the invariant catalytic triad residues: glutamate, lysine, and cysteine | Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
additional information | - |
greatly reduced activity observed at both acidic (pH 3.0) and basic (pH 10.0) conditions | Homo sapiens |
6.5 | 8 | - |
Homo sapiens |
7.5 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00404 | - |
pH 7.5, 25°C | Homo sapiens | 5-(N,N-Hexamethylene)amiloride | |
0.0057 | - |
pH 7.5, 25°C | Homo sapiens | 2,3-bis[(2-hydroxyethyl)thio]-1,4-naphthoquinone | |
0.0079 | - |
pH 7.5, 25°C | Homo sapiens | N2-(cis-2-aminocyclohexyl)-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine hydrochloride | |
0.0095 | - |
pH 7.5, 25°C | Homo sapiens | beta-lapachone | |
0.0135 | - |
pH 7.5, 25°C | Homo sapiens | 8-cyclopentyl-1,3-dipropylxanthine | |
0.0176 | - |
pH 7.5, 25°C | Homo sapiens | roscovitine |