Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition

Molecules

Duen-Ren Hou³  Ann-Chi Huang³  Chung-Wai Shiau¹  Chun-Yi Wang³  Hui-Chuan Yu² 

[1] Institute of Biopharmaceutical Sciences, National Yang-Ming University, Taipei 11221, Taiwan; E-Mail:;Department of Medical Research, National Taiwan University Hospital, Taipei 10048, Taiwan; E-Mail:;Department of Chemistry, National Central University, Taoyuan 32001, Taiwan; E-Mail:

关键词: CIP2A;    bortezomib;    apoptosis;   

DOI  :  10.3390/molecules181215398

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.