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FTY720 for cancer therapy (Review)
Li Zhang1, Han-Dong Wang, Xiang-Jun Ji
1Department of Neurosurgery, Jinling Hospital, School of Medicine, Nanjing University, Nanjing, Jiangsu 210002, P.R. China.
Abstract:
2-Amino-2-[2-(4-octylphenyl)]-1,3-propanediol hydrochloride (FTY720) is a potent immunosuppressant which has been approved by the Food and Drug Administration (FDA) as a new treatment for multiple sclerosis. As an immunosuppressant, it displays its anti-multiple sclerosis, immunosuppressive effects by activating sphingosine-1-phosphate receptors (S1PRs). In addition to the immunosuppressive effects, FTY720 also shows preclinical antitumor efficacy in several cancer models. In most cases, phosphorylation of FTY720 is not required for its cytotoxic effect, indicating the involvement of S1PR-independent mechanisms which are starkly different from the immunosuppressive property of FTY720. In the present study, we reviewed the rapidly advancing field of FTY720 in cancer therapy as well as some molecular targets of the unphosphorylated form of FTY720.
Insights
FTY720, an FDA-approved multiple sclerosis drug, also demonstrates preclinical antitumor effects. Unphosphorylated FTY720 targets cancer via S1PR-independent mechanisms, distinct from its immunosuppressive action.
Area of Science:
- Pharmacology
- Immunology
- Oncology
Background:
- 2-Amino-2-[2-(4-octylphenyl)]-1,3-propanediol hydrochloride (FTY720) is an FDA-approved immunosuppressant for multiple sclerosis.
- Its mechanism involves activating sphingosine-1-phosphate receptors (S1PRs).
- FTY720 exhibits preclinical antitumor efficacy in various cancer models.
Purpose of the Study:
- To review the therapeutic applications of FTY720 in cancer treatment.
- To explore the molecular targets of the unphosphorylated form of FTY720 in cancer therapy.
Main Methods:
- Literature review of FTY720 in cancer therapy.
- Analysis of S1PR-independent mechanisms of FTY720's cytotoxic effects.
Main Results:
- FTY720 demonstrates preclinical antitumor activity.
- Cytotoxic effects of FTY720 in cancer often do not require phosphorylation.
- These S1PR-independent mechanisms differ from its immunosuppressive properties.
Conclusions:
- FTY720 possesses dual therapeutic potential in multiple sclerosis and cancer.
- Understanding S1PR-independent pathways is crucial for FTY720's anticancer applications.
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