Pepstatin A

Pepstatin A is a potent aspartic protease inhibitor.Pepstatin A inhibits HIV replication.Pepstatin A is an irreversible inhibitor of aspartic proteases. Pepstatin A inhibits lysosomal proteases and interferes with autolysosomal digestion when used in combination with E 64d.Pepstatin and its derivatives inhibite other acid proteases, human pepsin, human gastricsin, renin, cathepsin D, the acid protease from Rhizopus chinensis and bovine chymosin. It is suggested that the statyl residue is responsible for the unusual inhibitory capability of pepstatin and that statine is an analog of the previously proposed transition state for catalysis by pepsin and other acid proteases.