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Publication detail

Novel potential proteasome inhibitors based on tripeptide scaffold

Authors: Dušek Jan | Imramovský Aleš

Year: 2014

Type of publication: ostatní - přednáška nebo poster

Page from-to: nestránkováno

Titles:

Language	Name	Abstract	Keywords
eng	Novel potential proteasome inhibitors based on tripeptide scaffold	Inhibition of proteasome via blocking its protein recycling function is one of a very promising ways to treat tumor cells or multiple myeloma. The most perspective inhibitors are carfilzomib (1, approved as Kyprolis®), bortezomib (2, approved as Velcade®) and MG132 (3). The potential inhibitors based on the salicylaic acid and tripeptide scaffold (4, O-benzyl-5-chlorosalicyl-tripeptides) were designed and synthesized. Due to a very similar constitution of mentioned novel compounds it can be expected very similar properties as well as biological activities. Prepared compounds are going to be tested as proteasomal and protein kinase inhibitors for the type of caused apoptosis.