Caged enzyme substrates as probes for reporter enzyme activity

摘要

Caged enzyme substrates as probes for detecting reporter enzyme activity in cell-based assays are disclosed. Caged substrates for reporter gene assays are shown as compounds of Formula I or Formula II: wherein Z is a luminescent functionality; G is a labile group, cleavable by enzymatic action; and K is a photolytically cleavable caging group; wherein m and n are independently 0 or 1, but m and n both can not be zero. Test kits for determining reporter enzyme activity using compounds of Formula I or Formula II and photolytic cleavage to produce a compound of Formula III:Gm-Z-GnIIIare described. Methods for determining reporter enzyme activity and, by inference, the activator or suppressor activity of a test compound in a cell-based assay are also described.