Integration of ERα-PELP1-HER2 signaling by LSD1 (KDM1A/AOF2) offers combinatorial therapeutic opportunities to circumventing hormone resistance in breast cancer

LSD1, an epigenetic modifier, and PELP1, an estrogen receptor co-activator, integrate estrogen receptor ERα and HER2 receptor tyrosine kinase signaling to promote aromatase expression and hormone resistance in a preclinical model of post-menopausal breast cancer. In the previous issue of Breast Canc...

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Bibliographic Details
Published in:Breast cancer research : BCR 2012-09, Vol.14 (5), p.112-112, Article 112
Main Author: Bennani-Baiti, Idriss M
Format: Article
Language:English
Subjects:
Animals
Breast Neoplasms - genetics
Breast Neoplasms - metabolism
Co-Repressor Proteins - genetics
Female
Histone Demethylases - metabolism
Humans
Transcription Factors - genetics
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Summary:LSD1, an epigenetic modifier, and PELP1, an estrogen receptor co-activator, integrate estrogen receptor ERα and HER2 receptor tyrosine kinase signaling to promote aromatase expression and hormone resistance in a preclinical model of post-menopausal breast cancer. In the previous issue of Breast Cancer Research, Cortez et al. show, for the first time, that knockdown or drug-mediated inhibition of PELP1 or LSD1 suppresses LSD1-mediated transcriptionally activating histone marks at ERα target genes, inhibits aromatase gene expression, and sensitizes hormone refractory breast cancer cells to tamoxifen or letrozole treatments. The relevance of PELP1-LSD1 signaling to other nuclear hormone receptor-dependent cancers and structural considerations for the selective drug targeting of LSD1 are further discussed in this editorial.
ISSN:1465-5411
1465-542X
1465-542X
DOI:10.1186/bcr3249