Transcriptomics,Genomics

Dataset Information

28

The phosphorylated prodrug FTY720 is a histone deacetylase Q15 inhibitor that reactivates ERα expression and enhances hormonal therapy for breast cancer


ABSTRACT: Nuclear FTY720-P is a potent inhibitor of class I histone deacetylases (HDACs) that enhances histone acetylations and regulates expression of a restricted set of genes independently of its known effects on canonical signaling through sphingosine-1-phosphate (S1P) receptors. We found that FTY720 is phosphorylated in Era-negative breast cancer cells by nuclear sphingosine kinase 2 and accumulates these cells. Overall design: To determine whether FTY720-P inhibits HDACs in Era-negative breast cancer cells and in tumors to regulate histone acetylation and gene expression, and it can re-express ERα in these aggressive breast carcinoma for hormonal therapies.

INSTRUMENT(S): [HG-U133A_2] Affymetrix Human Genome U133A 2.0 Array

SUBMITTER: Catherine Dumur 

PROVIDER: GSE69462 | GEO | 2015-06-03

SECONDARY ACCESSION(S): PRJNA285668

REPOSITORIES: GEO

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Publications

The phosphorylated prodrug FTY720 is a histone deacetylase inhibitor that reactivates ERα expression and enhances hormonal therapy for breast cancer.

Hait N C NC   Avni D D   Yamada A A   Nagahashi M M   Aoyagi T T   Aoki H H   Dumur C I CI   Zelenko Z Z   Gallagher E J EJ   Leroith D D   Milstien S S   Takabe K K   Spiegel S S  

Oncogenesis 20150608


Estrogen receptor-α (ERα)-negative breast cancer is clinically aggressive and does not respond to conventional hormonal therapies. Strategies that lead to re-expression of ERα could sensitize ERα-negative breast cancers to selective ER modulators. FTY720 (fingolimod, Gilenya), a sphingosine analog, is the Food and Drug Administration (FDA)-approved prodrug for treatment of multiple sclerosis that also has anticancer actions that are not yet well understood. We found that FTY720 is phosphorylated  ...[more]

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