Synthesis and biological properties of C-terminal vinyl ketone pseudotripeptides. (June 2013)

• Record Type: Journal Article
• Authors: Franceschini, Christian; Trapella, Claudio; Sforza, Fabio; Gavioli, Riccardo; Marastoni, Mauro
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 28:Number 3(2013:Jun.)
• Page Start: 560
• Page End: 564
• Publication Date: 2013-06
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2012.657189
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title> <x xml:space="preserve">Abstract</x> </title> <p>The ubiquitin-proteasome pathway responsible for the turnover of many cellular proteins represents an attractive target in the development of new drug therapies: In particular, modulation of the proteasome activity by specific inhibitors may represent a useful tool for the treatment of tumours. Here, we report synthesis and activity of a new series of oligopseudopeptide analogues bearing a vinyl ketone pharmacophoric unit at the C-terminal position. Some derivatives showed inhibition in the µM range of the trypsin-like (T-L) active site of the proteasome.</p> </abstract>