Mechanism-based inactivation of E. coli γ-glutamylcysteine synthetase by phosphinic acid- and sulfoximine-based transition-state analogues

Article abstract of DOI:10.1016/S0960-894X(96)00247-8

Phosphinic acid- and sulfoximine-based transition state analogues having a carboxyl group at the β-carbon to the hetero atom exhibited significantly higher potency as mechanism-based inhibitors of E. coli γ-glutamylcysteine synthetase as compared with L-buthionine-SR-sulfoximine. The enhanced inhibition potency is evidenced by both tight binding of the inhibitor and slow enzyme reactivation.