Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.5.3.1 extracted from

  • Nau, W.M.; Ghale, G.; Hennig, A.; Bakirci, H.; Bailey, D.M.
    Substrate-selective supramolecular tandem assays: monitoring enzyme inhibition of arginase and diamine oxidase by fluorescent dye displacement from calixarene and cucurbituril macrocycles (2009), J. Am. Chem. Soc., 131, 11558-11570.
    View publication on PubMed

Application

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

Inhibitors Comment Organism Structure
2-(S)-amino-6-boronohexanoic acid
-
Bos taurus
S-(2-boronoethyl)-L-cysteine
-
Bos taurus

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Bos taurus
-
liver
-
Bos taurus
-

Ki Value [mM]

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 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