Pepstatin is a pentapeptide, a naturally occurring aspartyl protease inhibitor, which can inhibit aspartic protease and acid protease of various microorganisms. Pepstatin is mainly secreted by Streptomyces species and produced by Streptomyces. It can inhibit pepsin, pepsin D and angiotensin-releasing enzyme, and has therapeutic effects on gastric ulcer, renal hypertension, arthritis, carrageenan edema and other diseases.
Pepstatin is a strong inhibitor of aspartyl proteases such as pepsin, cathepsin D, and renin. This natural pentapeptide isolated from actinomycetes was for many years the classic renin inhibitor in vitro.Pepstatin is not specific for renin and is poorly soluble in water. Structural derivatives of pepstatin increased its solubility and specificity for renin by several orders of magnitude.Pepstatin contains the unusual γ amino acid statin that may substitute for the two amino acids at the scissile bond of theprotein substrate and block substrate cleavage because of the structural analogy to a transition state of the peptide bond hydrolysis by aspartyl proteases.
