Peptidyl Aldehyde Specifically Interacts with Immunosubunit β1i Proteasome: In Vitro and In Vivo Effects.

We studied the effect of β1i-specific peptidyl aldehyde IPSI-001 on proteasome from mammalian cells. In concentrations <1 μM, this agent effectively suppressed immunoproteasome, but only slightly reduced chymotrypsin-like activity of constitutive proteasome. Intraperitoneal administration of this inhibitor to C3H/He mice in a dose of 100 mg/kg induced no significant physiological or behavioral changes, which attested to its considerable therapeutic potential in the treatment of autoimmune neurodegenerative pathologies.