Bortezomib congeners induce apoptosis of hepatocellular carcinoma via CIP2A inhibition

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Title:	Bortezomib congeners induce apoptosis of hepatocellular carcinoma via CIP2A inhibition
Authors:	侯敦仁;Hou, Duen-Ren;Huang, Ann-Chi;Shiau, Chung-Wai;Wang, Chun-Yi;Yu, Hui-Chuan;Chen, Kuen-Feng
Contributors:	理學院化學學系
Keywords:	Acids;Antineoplastic Agents - chemical synthesis;Antineoplastic Agents - chemistry;Antineoplastic Agents - pharmacology;Apoptosis;Apoptosis - drug effects;Autoantigens - genetics;Autoantigens - metabolism;Boronic Acids - chemical synthesis;Boronic Acids - chemistry;Boronic Acids - pharmacology;Bortezomib;Carcinoma, Hepatocellular - genetics;Carcinoma, Hepatocellular - metabolism;Cell growth;Cell Line, Tumor;Cell Proliferation - drug effects;Cell Survival - drug effects;CIP2A;Gene Knockdown Techniques;Humans;Hydrogen;Inhibitory Concentration 50;Liver cancer;Liver Neoplasms - genetics;Liver Neoplasms - metabolism;Membrane Proteins - antagonists & inhibitors;Membrane Proteins - genetics;Membrane Proteins - metabolism;Molecular Structure;Natural products;Phosphatase;Pyrazines - chemical synthesis;Pyrazines - chemistry;Pyrazines - pharmacology;Structure-Activity Relationship;Toxicity
Date:	2013-12-01
Issue Date:	2026-04-21 14:16:18 (UTC+8)
Publisher:	MDPI Multidisciplinary Digital Publishing Institute;Switzerland: MDPI AG
Abstract:	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. 其他題名： Molecules 出版者： Switzerland: MDPI AG 出版日期： 2013-12-11 出處： Molecules, 2013-12, Vol.18 (12), p.15398-15411 資源來源： Publicly Available Content Database 版權： Copyright MDPI AG 2013 版權： 2013 by the authors; licensee MDPI, Basel, Switzerland. 2013 識別號： ISSN: 1420-3049 識別號： ISSN: 1433-1373 識別號： EISSN: 1420-3049 識別號： EISSN: 1433-1373 識別號： DOI: 10.3390/molecules181215398 識別號： PMID: 24335617
Appears in Collections:	[Department of Chemistry] journal & Dissertation

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