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Bortezomib congeners induce apoptosis of hepatocellular carcinoma via CIP2A inhibition.

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.

SUBMITTER: Hou DR 

PROVIDER: S-EPMC6269665 | biostudies-literature | 2013 Dec

REPOSITORIES: biostudies-literature

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Bortezomib congeners induce apoptosis of hepatocellular carcinoma via CIP2A inhibition.

Hou Duen-Ren DR   Huang Ann-Chi AC   Shiau Chung-Wai CW   Wang Chun-Yi CY   Yu Hui-Chuan HC   Chen Kuen-Feng KF  

Molecules (Basel, Switzerland) 20131211 12

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 i  ...[more]

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