Provided herein is a crystallized ternary structure of human aldose
reductase (AR) bound to NADPH and
.gamma.-glutamyl-S-(1,2-dicarboxyethyl)cysteinylglycine (DCEG). Also
provided are specific inhibitors of glutathione-aldehyde binding to
aldose reductase which are designed via at least computer modeling of the
ternary AR:NADPH:DCEG structure and methods of designing and of screening
the inhibitors for inhibition of glutathione-aldehyde binding to aldose
reductase.