| Assay Method Information | |
| | Enzymatic Activity of Human Glutaminyl Cyclase In Vitro |
| Description: | During studies of the effect of Compounds I-X, which are the object of the present invention, on the enzymatic activity of glutaminyl cyclase in vitro, the direct inhibitory effect of Compounds I-X on recombinant intracellular human glutaminyl cyclase first has been found. The glutaminyl cyclase activity at various concentrations of Compounds I-X has been studied at 25 C. with the use of a fluorescent substrate L-glutaminyl 2-naphthyl amide (Gln-bNA) (Anal Biochem. 2002 Apr. 1; 303(1):49-56). The reaction mixture having a volume of 100-μl has contained 50 μM of fluorogenic substrate; 0.2 units of human pyroglutaminyl aminopeptidase (1 unit is defined as an amount hydrolyzing 1 micromole of pGlu-bNA per minute), and an aliquot of the recombinant intracellular human glutaminyl cyclase (gQC) in 50 mM trisaminomethane-HCl and 5% glycerol, a pH is 8.0. The reaction was initiated by adding to the reaction mixture an aliquot of glutaminyl cyclase incubated with Compounds I-X for 5 minutes. |
| Affinity data for this assay | |
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