Glutathione S-transferase (GST) are phase II enzymes that catalyze the nucleophilic attack of glutathione (GSH) to a wide range of hydrophobic and electrophilic compounds. GST is known to highly express in cancer cells. Therefore, we tried to develop new luminogenic probes that can detect and image GST expression in living cells. Recently, we found that the electrophilic centre in the dinitrobenzenesulfonamide derivative is attacked by GSH and that this reaction is catalyzed by GST releasing the strong fluorophore. Based on this knowledge, we synthesized fluorogenic probe and bioluminogenic probe. The fluorescent probe and kinetic parameters for purified GST were giving a rate enhancement of 106 compared with the nonenzymatic reaction. In addition, fluorogenic probe successfully image GST in living cells. The fluorescent probe is potentially useful reagent for detection of GST activity in living cells. For the future, the bioluminogenic probe is tested whether luminescence appears by GST activity.

Development of new luminogenic probes for detection of glutathione s-transferase activity in living cells

244th National Meeting (2012)

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