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


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Abstract

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.

About the authors

E. S. Kuzina

M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences

Email: belogurov@mx.ibch.ru
Russian Federation, Moscow

A. A. Kudriaeva

M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences

Email: belogurov@mx.ibch.ru
Russian Federation, Moscow

D. V. Maltseva

BioClinicum Research and Development Center

Email: belogurov@mx.ibch.ru
Russian Federation, Moscow

A. A. Belogurov

M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences

Author for correspondence.
Email: belogurov@mx.ibch.ru
Russian Federation, Moscow


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