Synthesis of Novel FTY720 Analogs with Anticancer Activity through PP2A Activation
- Authors
- Shrestha, Jitendra; Ki, Sung Hwan; Shin, Sang Mi; Kim, Seon Woong; Lee, Joo-Youn; Jun, Hee-Sook; Lee, Taeho; Kim, Sanghee; Baek, Dong Jae; Park, Eun-Young
- Issue Date
- Nov-2018
- Publisher
- MDPI
- Keywords
- FTY720; protein phosphatase 2A; sphingosine kinase; colorectal cancer; derivative
- Citation
- MOLECULES, v.23, no.11
- Journal Title
- MOLECULES
- Volume
- 23
- Number
- 11
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/3132
- DOI
- 10.3390/molecules23112750
- ISSN
- 1420-3049
- Abstract
- FTY720 inhibits various cancers through PP2A activation. The structure of FTY720 is also used as a basic structure for the design of sphingosine kinase (SK) inhibitors. We have synthesized derivatives using an amide chain in FTY720 with a phenyl backbone, and then compounds were screened by an MTT cell viability assay. The PP2A activity of compound 7 was examined. The phosphorylation levels of AKT and ERK, downstream targets of PP2A, in the presence of compound 7, were determined. Compound 7 may exhibit anticancer effects through PP2A activation rather than the mechanism by inhibition of SK1 in cancer cells. In the docking study of compound 7 and PP2A, the amide chain of compound 7 showed an interaction with Asn61 that was different from FTY720, which is expected to affect the activity of the compound.
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