Bortezomib congeners induce apoptosis of hepatocellular carcinoma via CIP2A inhibition

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Duen-Ren HouKuen-Feng Chen

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.

References

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Citations

Jan 30, 2015·International Journal of Cancer. Journal International Du Cancer·Anchit Khanna, John E Pimanda
Nov 7, 2017·The International Journal of Biochemistry & Cell Biology·Caitlin M O'ConnorGoutham Narla

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Methods Mentioned

BETA
ELISA
flow cytometry
nuclear magnetic resonance
column chromatography
Assay

Software Mentioned

VisionWork LS

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