Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2024;24(3):192-200.
doi: 10.2174/0115680266273421231222061620.

Pharmacological Effects of FTY720 and its Derivatives

Affiliations
Review

Pharmacological Effects of FTY720 and its Derivatives

Mengyuan Han et al. Curr Top Med Chem. 2024.

Abstract

FTY720 is an analog of sphingosine-1-phosphate (S1P) derived from the ascomycete Cordyceps sinensis. As a new immunosuppressant, FTY720 is widely used to treat multiple sclerosis. FTY720 binds to the S1P receptor after phosphorylation, thereby exerting immunosuppressive effects. The nonphosphorylated form of FTY720 can induce cell apoptosis, enhance chemotherapy sensitivity, and inhibit tumor metastasis of multiple tumors by inhibiting SPHK1 (sphingosine kinase 1) and activating PP2A (protein phosphatase 2A) and various cell death pathways. FTY720 can induce neutrophil extracellular traps to neutralize and kill pathogens in vitro, thus exerting anti- infective effects. At present, a series of FTY720 derivatives, which have pharmacological effects such as anti-tumor and alleviating airway hyperresponsiveness, have been developed through structural modification. This article reviews the pharmacological effects of FTY720 and its derivatives.

Keywords: Anti-infection; Anti-tumor; Derivative; FTY720; Immunosuppression; Pharmacological effects..

PubMed Disclaimer

Similar articles

Cited by

References

    1. (a) Fujita T.; Matsumoto N.; Uchida S.; Kohno T.; Shimizu T.; Hirose R.; Yanada K.; Kurio W.; Watabe K.; Antibody against a novel, myriocin (ISP-I)-Based immunosuppressant, FTY720. Bioorg Med Chem Lett 2000,10(4),337-339 - DOI - PubMed
    1. (b) Fujita T, Inoue K, Yamamoto S, Ikumoto T, Sasaki S, Toyama R, Chiba K, Hoshino Y, Okumoto T.; Fungal metabolites. part 11. A potent immunosuppressive activity found in isaria sinclairii metabolite. J Antibiot 1994,47,208-15 - DOI - PubMed
    1. (c) Fujita T, Hamamichi N, Kiuchi M, Matsuzaki T, Kitao Y, Inoue K, Hirose R, Yoneta M, Sasaki S, Chiba K.; Determination of absolute configuration and biological activity of new immunosuppressants, mycestericins D, E, F and G. J Antibiot Erratum in: J Antibiot (Tokyo) 1996 Dec;49(12):C-31996,49,846-53 - DOI - PubMed
    1. Brinkmann V.; Davis M.D.; Heise C.E.; Albert R.; Cottens S.; Hof R.; Bruns C.; Prieschl E.; Baumruker T.; Hiestand P.; Foster C.A.; Zollinger M.; Lynch K.R.; The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem 2002,277(24),21453-21457 - DOI - PubMed
    1. Suzuki S.; Ogawa M.; Miyazaki M.; Ota K.; Kazama H.; Hirota A.; Takano N.; Hiramoto M.; Miyazawa K.; Lysosome-targeted drug combination induces multiple organelle dysfunctions and non-canonical death in pancreatic cancer cells. Oncol Rep 2021,47(2),40 - DOI - PubMed

MeSH terms

Substances

LinkOut - more resources