Document Report Card

ID: ALA1149108

Journal: J Med Chem

Title: Arecoline tripeptide inhibitors of proteasome.

Authors: Marastoni M, Baldisserotto A, Canella A, Gavioli R, Risi CD, Pollini GP, Tomatis R.

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.

CiteXplore: 14998343

DOI: 10.1021/jm0309102