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Updated: Aug 26, 2026

Examining Proteasome Assembly with Recombinant Archaeal Proteasomes and Nondenaturing PAGE: The Case for a Combined Approach
Published on: December 17, 2016
Arecoline tripeptide inhibitors of proteasome
Mauro Marastoni1, Anna Baldisserotto, Alessandro Canella
1Department of Pharmaceutical Sciences and Biotechnology Center, and Department of Biochemistry and Molecular Biology, University of Ferrara, I-44100 Ferrara, Italy. mru@unife.it
Abstract:
The 26S proteasome is a multicatalytic protease complex that plays an essential role in intracellular protein degradation. We have synthesized and tested a series of arecoline peptide derivatives where the peptide portion derives from a screening of tripeptide sequences, and the arecoline moiety has been considered as a potential substrate for catalytic threonine. Derivatives 17-19 are the best compounds of the series, showing chymotryptic-like (beta5) inhibition (IC(50) congruent with 1 microM) and favorable pharmacokinetic properties.
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