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  • Title: Arecoline tripeptide inhibitors of proteasome.
    Author: Marastoni M, Baldisserotto A, Canella A, Gavioli R, Risi CD, Pollini GP, Tomatis R.
    Journal: J Med Chem; 2004 Mar 11; 47(6):1587-90. PubMed ID: 14998343.
    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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