Discovery at the interface: Toward novel anti-proliferative agents targeting human estrogen receptor/S100 interactions.

ABSTRACT: Estrogen Receptor Alpha (ER) is expressed in about 70% of breast cancer and mediates various cellular signaling events including cell cycle. The antiestrogen tamoxifen is currently administered to patients in order to induce regression of the tumor growth of estrogen receptor positive (ER+) breast cancer. However, upon continued administration, patients develop resistance to tamoxifen. In addition, calcium binding proteins (EF-hand proteins) such as, Calmodulin and S100, are significantly overexpressed in breast cancer cells, can activate transcription of target genes by directly binding to ER in lieu of estrogen. Calmodulin antagonists (w7 and melatonin) have been shown to significantly inhibit ER mediated activities including cell proliferation and transcriptional activity. Furthermore,

SUBMITTER: Lee DH 

PROVIDER: S-EPMC5053565 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature