The glyoxalase enzyme system is highly conserved among all organisms and plays a key role in detoxifying the cytotoxic metabolite methylglyoxal into lactic acid. Glyoxalase I (GxI) is considered an anticancer target because inhibiting the enzyme will result in a localized buildup of methylglyoxal, which can potentially induce cell death in those targeted cells. This research focused on an evaluation of the conjugate between glutathione (GSH) and 3-methyleneoxindole (GSMOI) as a potential inhibitor of human GxI. GSMOI were synthesized and characterized, and subsequently tested as a competitive inhibitor for both yeast and human GxI. In contrast to previous research on GSH conjugates, this work suggests that GSMOI inhibits yeast GxI through mixed inhibition instead of pure competitive. It was also found that GSMOI is an inhibitor of human GxI, and preliminary results suggest irreversible time-dependent inactivation is occurring.

Synthesis and evaluation of the glutathione-3-methyleneoxindole conjugate as a potential inhibitor of human glyoxalase I

245th National Meeting (2013)

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