https://scholars.lib.ntu.edu.tw/handle/123456789/375898
標題: | Bortezomib congeners induce apoptosis of hepatocellular carcinoma via CIP2A inhibition | 作者: | Kuen-Feng Chen | 關鍵字: | Apoptosis; Bortezomib; CIP2A | 公開日期: | 2013 | 卷: | 18 | 期: | 12 | 起(迄)頁: | 15398-15411 | 來源出版物: | Molecules | 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. ? 2013 by the authors; licensee MDPI, Basel, Switzerland. |
URI: | http://www.scopus.com/inward/record.url?eid=2-s2.0-84890904236&partnerID=MN8TOARS http://scholars.lib.ntu.edu.tw/handle/123456789/375898 |
DOI: | 10.3390/molecules181215398 | SDG/關鍵字: | antineoplastic agent; autoantigen; boronic acid derivative; bortezomib; KIAA1524 protein, human; membrane protein; pyrazine derivative; apoptosis; article; cell proliferation; cell survival; chemical structure; chemistry; drug antagonism; drug effect; gene silencing; genetics; human; IC 50; liver cell carcinoma; liver tumor; metabolism; structure activity relation; synthesis; tumor cell line; Antineoplastic Agents; Apoptosis; Autoantigens; Boronic Acids; Carcinoma, Hepatocellular; Cell Line, Tumor; Cell Proliferation; Cell Survival; Gene Knockdown Techniques; Humans; Inhibitory Concentration 50; Liver Neoplasms; Membrane Proteins; Molecular Structure; Pyrazines; Structure-Activity Relationship |
顯示於: | 醫學系 |
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