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.
Marastoni, Mauro; Baldisserotto, Anna; Canella, Alessandro; Gavioli, Riccardo; DE RISI, Carmela; Pollini, Gian Piero; Tomatis, Roberto
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/1196694
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