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Bioorg Med Chem. 2013 Jan 1;21(1):311-20. doi: 10.1016/j.bmc.2012.10.037. Epub 2012 Oct 29.

Ridaifen B, a tamoxifen derivative, directly binds to Grb10 interacting GYF protein 2.

Author information

1
Department of Applied Biological Science, Faculty of Science and Technology, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.

Abstract

Ridaifen B (RID-B) is a tamoxifen derivative that potently inhibits breast tumor growth. RID-B was reported to show anti-proliferating activity for a variety of estrogen receptor (ER)-positive human cancer cells. Interestingly, RID-B was also reported to possess higher potency than that of tamoxifen even for some ER-negative cells, suggesting an ER-independent mechanism of action. In this study, a T7 phage display screen and subsequent binding analyses have identified Grb10 interacting GYF protein 2 (GIGYF2) as a RID-B-binding protein. Using a cell-based assay, the Akt phosphorylation level mediated by GIGYF2 was found to have decreased in the presence of RID-B.

PMID:
23199482
DOI:
10.1016/j.bmc.2012.10.037
[Indexed for MEDLINE]

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