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 (â5) inhibition (IC50 = 1 íM) and favorable pharmacokinetic properties.
Arecoline tripeptide inhibitors of proteasome
MARASTONI, Mauro;BALDISSEROTTO, Anna;CANELLA, Alessandro;GAVIOLI, Riccardo;DE RISI, Carmela;POLLINI, Gian Piero;TOMATIS, Roberto
2004
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 (â5) inhibition (IC50 = 1 íM) and favorable pharmacokinetic properties.File in questo prodotto:
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