Abstract
Sialylation of glycoproteins and glycolipids plays an important role in many cell surface processes; of special interest in this context are changes in tissue involved in diseases and especially changes during infections. Therefore, inhibitors of sialyltransferases regulating sialylation might be of medicinal interest, especially in the therapy of virus and cancer diseases. The present paper reviews the development of sialyltransferase inhibitors; thus acceptor analogs, donor analogs, transition-state analogs, and bisubstrate analogs were designed based on sialic acid derivatives as well as on structural mimetics. This way, very potent sialyltransferase inhibitors with inhibition constants in the low nanomolar range have been recently found.
