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Ridaifen B, a Tamoxifen Derivative, Directly Binds to Grb10 Interacting GYF Protein 2

Ridaifen B, a Tamoxifen Derivative, Directly Binds to Grb10 Interacting GYF Protein 2

Senko Tsukuda, Tomoe Kusayanagi, Eri Umeda, Chihiro Watanabe, Yu-ta Tosaki, Shinji Kamisuki, Toshifumi Takeuchi, Yoichi Takakusagi, Isamu Shiina, Fumio Sugawara

Bioorg Med Chem. 2013 Jan 1;21(1):311-20.

PMID: 23199482

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP886465709	Ridaifen-B		886465-70-9	Price

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