Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition
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 conducte...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2013-12-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/18/12/15398 |
| _version_ | 1818465764247601152 |
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| author | Duen-Ren Hou Ann-Chi Huang Chung-Wai Shiau Chun-Yi Wang Hui-Chuan Yu Kuen-Feng Chen |
| author_facet | Duen-Ren Hou Ann-Chi Huang Chung-Wai Shiau Chun-Yi Wang Hui-Chuan Yu Kuen-Feng Chen |
| author_sort | Duen-Ren Hou |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-13T20:49:55Z |
| format | Article |
| id | doaj.art-96081d779ad7476eb27965052032d431 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-04-13T20:49:55Z |
| publishDate | 2013-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-96081d779ad7476eb27965052032d4312022-12-22T02:30:33ZengMDPI AGMolecules1420-30492013-12-011812153981541110.3390/molecules181215398molecules181215398Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A InhibitionDuen-Ren Hou0Ann-Chi Huang1Chung-Wai Shiau2Chun-Yi Wang3Hui-Chuan Yu4Kuen-Feng Chen5Department of Chemistry, National Central University, Taoyuan 32001, TaiwanDepartment of Chemistry, National Central University, Taoyuan 32001, TaiwanInstitute of Biopharmaceutical Sciences, National Yang-Ming University, Taipei 11221, TaiwanDepartment of Chemistry, National Central University, Taoyuan 32001, TaiwanDepartment of Medical Research, National Taiwan University Hospital, Taipei 10048, TaiwanDepartment of Medical Research, National Taiwan University Hospital, Taipei 10048, TaiwanCIP2A 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.http://www.mdpi.com/1420-3049/18/12/15398CIP2Abortezomibapoptosis |
| spellingShingle | Duen-Ren Hou Ann-Chi Huang Chung-Wai Shiau Chun-Yi Wang Hui-Chuan Yu Kuen-Feng Chen Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition Molecules CIP2A bortezomib apoptosis |
| title | Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition |
| title_full | Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition |
| title_fullStr | Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition |
| title_full_unstemmed | Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition |
| title_short | Bortezomib Congeners Induce Apoptosis of Hepatocellular Carcinoma via CIP2A Inhibition |
| title_sort | bortezomib congeners induce apoptosis of hepatocellular carcinoma via cip2a inhibition |
| topic | CIP2A bortezomib apoptosis |
| url | http://www.mdpi.com/1420-3049/18/12/15398 |
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