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The characterization of the transition state structure of a number of N-ribosyltransferases has enabled the design and synthesis of some extremely powerful inhibitors of these enzymes. We have three generations of inhibitors for some nucleoside processing enzymes which are therapeutic targets, and the potency of these compounds confers special advantages in their development as new drugs against cancer, autoimmune diseases, microbial infections and malaria.

Transition State Analogue Inhibitors of N-Ribosyltransferases: New Drugs by Targeting Nucleoside Processing Enzymes.