MDPI Multidisciplinary Digital Publishing Institute;Switzerland: MDPI AG
摘要:
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