Application | Comment | Organism |
---|---|---|
analysis | assay method based on a combination of moderately selective host-guest binding with the specificity of enzymatic transformations which allows the real-time monitoring of enzymatic reactions in a homogeneous solution. The resulting supramolecular tandem assays exploit the dynamic binding of a fluorescent dye with a macrocyclic host in competition with the binding of the substrate and product. The depletion of the substrate allows the fluorescent dye to enter the macrocycle in the course of the enzymatic reaction, which leads to the desired fluorescence response. For arginase, p-sulfonatocalix[4]arene is used as the macrocycle, which displays binding constants of 6400 per M with arginine, 550 per M with ornithine, and 60 000 per M with the selected fluorescent dye 1-aminomethyl-2,3-diazabicyclo[2.2.2]oct-2-ene, the dye shows a weaker fluorescence in its complexed state, which leads to a switch-off fluorescence response in the course of the enzymatic reaction. Assays can be successfully used to probe the inhibition of enzymes | Bos taurus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-(S)-amino-6-boronohexanoic acid | - |
Bos taurus | |
S-(2-boronoethyl)-L-cysteine | - |
Bos taurus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Bos taurus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
commercial preparation | - |
Bos taurus | - |
liver | - |
Bos taurus | - |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00015 | - |
2-(S)-amino-6-boronohexanoic acid | pH 9.5, 25°C, supramolecular tandem assay method | Bos taurus | |
0.0036 | - |
S-(2-boronoethyl)-L-cysteine | pH 9.5, 25°C, supramolecular tandem assay method | Bos taurus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00022 | - |
pH 9.5, 25°C, supramolecular tandem assay method | Bos taurus | 2-(S)-amino-6-boronohexanoic acid | |
0.0037 | - |
pH 9.5, 25°C, supramolecular tandem assay method | Bos taurus | S-(2-boronoethyl)-L-cysteine |