Bortezomib congeners induce apoptosis of hepatocellular carcinoma via CIP2A inhibition

Duen Ren Hou, Ann Chi Huang, Chung Wai Shiau, Chun Yi Wang, Hui Chuan Yu, Kuen Feng Chen

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

CIP2A is an oncoprotein that upregulates p-Akt and promotes cancer cell proliferation and survival. The proteasome inhibitor bortezomib has been shown to reduce CIP2A and lead to cell apoptosis. Here; we modified the functional group of bortezomib to generate a series of novel compounds and conducted a structure-activity relationship (SAR) study. The results showed that compound 1 was able to repress CIP2A expression and cell apoptosis in the same manner as bortezomib, but with less potency in inhibition of proteasome activity. This finding provides a new direction for the design of CIP2A inhibitors.

Original languageEnglish
Pages (from-to)15398-15411
Number of pages14
JournalMolecules
Volume18
Issue number12
DOIs
StatePublished - Dec 2013

Keywords

  • Apoptosis
  • Bortezomib
  • CIP2A

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