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Cancer-related γ-glutamyl cyclotransferase (GGCT) specifically converts γ-glutamyl amino acids (γ-Glu-Xaa) into pyroglutamate and the corresponding amino acids (Xaa). Here we report a novel GGCT fluorogenic probe “LISA-101” containing a masked O-acylated fluorophore “resorufin” on the side chain of the P1 amino acid (Xaa). Upon GGCT treatment, the P1 amino acid was liberated and spontaneously released the intact fluorophore. Thus, the fluorescence was regained. LISA-101 will expand the strategies for cancer studies.

Graphical abstract: A GGCT fluorogenic probe: design, synthesis and application to cancer-related cells

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