A GIGYF2 modulator including, as an active ingredient, a compound represented by the following Formula (I): wherein, in Formula (I), R1 and R2 each independently represent a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms, or R1 and R2 may bind together to form a cyclic group with a nitrogen atom attached thereto; and n represents an integer from 2 to 6.
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(2014/05/07)
Ridaifen B, a tamoxifen derivative, directly binds to Grb10 interacting GYF protein 2
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.