Document Report Card

ID: ALA2150851

Journal: J Med Chem

Title: Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.

Authors: Frizler M, Schmitz J, Schulz-Fincke AC, Gütschow M.

Abstract: A series of dipeptide nitriles with different P3 substituents was designed to explore the S3 binding pocket of cathepsin S. Racemic 7-16 and the enantiopure derivative (R)-22 proved to be potent inhibitors of human cathepsin S and exhibited notable selectivity over human cathepsins L, K, and B. Inhibition of cathepsin F, the functional synergist of cathepsin S, was not observed. The azadipeptide analogue of 22, compound 26, was highly potent but nonselective.

CiteXplore: 22686657

DOI: 10.1021/jm300734k