Molecules 2013, 18(12), 15398-15411; doi:10.3390/molecules181215398
Article

Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition

1,†email, 1,†email, 2,†email, 1email, 3,4email and 3,4,* email
Received: 25 August 2013; in revised form: 20 November 2013 / Accepted: 28 November 2013 / Published: 11 December 2013
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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.
Keywords: CIP2A; bortezomib; apoptosis
PDF Full-text Download PDF Full-Text [1074 KB, uploaded 18 June 2014 20:16 CEST]

Export to BibTeX |
EndNote


MDPI and ACS Style

Hou, D.-R.; Huang, A.-C.; Shiau, C.-W.; Wang, C.-Y.; Yu, H.-C.; Chen, K.-F. Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition. Molecules 2013, 18, 15398-15411.

AMA Style

Hou D-R, Huang A-C, Shiau C-W, Wang C-Y, Yu H-C, Chen K-F. Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition. Molecules. 2013; 18(12):15398-15411.

Chicago/Turabian Style

Hou, Duen-Ren; Huang, Ann-Chi; Shiau, Chung-Wai; Wang, Chun-Yi; Yu, Hui-Chuan; Chen, Kuen-Feng. 2013. "Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition." Molecules 18, no. 12: 15398-15411.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert