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Updated: Mar 24, 2026

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Potential anti-tumor effects of FTY720 associated with PP2A activation: a brief review
Ion Cristóbal1, Juan Madoz-Gúrpide2, Rebeca Manso2
1a Translational Oncology Division , Oncohealth Institute, IIS-Fundacion Jimenez Diaz-UAM, University Hospital 'Fundacion Jimenez Diaz' , Madrid , Spain ;
Abstract:
FTY720 (Fingolimod, Gilenya (†) ) is an FDA-approved immunosuppressant currently used in the treatment of multiple sclerosis. However, a large number of studies over the last few years have shown that FTY720 shows potent antitumor properties that suggest its potential usefulness as a novel anticancer agent. Interestingly, the restoration of protein phosphatase 2A (PP2A) activity mediated by FTY720 could play a key role in its antitumor effects. Taking into account that PP2A inactivation is a common event that determines poor outcome in several tumor types, FTY720 could serve as an alternative therapeutic strategy for cancer patients with such alterations.
Insights
FTY720 (Fingolimod) is an immunosuppressant that shows potent anticancer properties. It may be a novel therapeutic strategy for cancer by restoring protein phosphatase 2A (PP2A) activity.
Area of Science:
- Oncology
- Immunology
- Pharmacology
Background:
- FTY720 (Fingolimod) is an FDA-approved immunosuppressant for multiple sclerosis.
- Emerging research indicates FTY720 possesses significant antitumor properties.
- PP2A inactivation is linked to poor prognosis in various cancers.
Purpose of the Study:
- To explore the potential of FTY720 as a novel anticancer agent.
- To investigate the role of protein phosphatase 2A (PP2A) activity in FTY720's antitumor effects.
Main Methods:
- Review of existing studies on FTY720's pharmacological and antitumor activities.
- Analysis of the mechanism linking FTY720 to PP2A activity restoration.
Main Results:
- FTY720 demonstrates potent anticancer effects in preclinical studies.
- Restoration of PP2A activity by FTY720 is a key mechanism underlying its antitumor action.
Conclusions:
- FTY720 shows promise as a novel therapeutic agent for cancer treatment.
- Its ability to restore PP2A activity offers a potential strategy for cancers with PP2A alterations.
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