Development of novel peptidomimetics containing a vinyl sulfone moiety as proteasome inhibitors

R Ettari, C Bonaccorso, N Micale, C Heindl…

Index: Ettari, Roberta; Bonaccorso, Cinzia; Micale, Nicola; Heindl, Cornelia; Schirmeister, Tanja; Calabro, Maria Luisa; Grasso, Silvana; Zappala, Maria ChemMedChem, 2011 , vol. 6, # 7 p. 1228 - 1237

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Citation Number: 20

Abstract

Abstract Proteasome inhibition is a topic of great interest in anticancer research. The proteolytic activity of this multicatalytic complex relies on three subunits, β1, β2 and β5, containing a caspase-like, a trypsin-like and a chymotrypsin-like active site, respectively. Several studies have demonstrated that, of the three activities, the chymotrypsin-like activity was the most necessary for cell viability and protein processing. Thus, most efforts towards ...