title: Ridaifen B, a tamoxifen derivative, directly binds to Grb10 interacting GYF protein 2.
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.
authors.affiliation: Department of Applied Biological Science, Faculty of Science and Technology, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
authors.forename: Senko
authors.initials: S
authors.lastname: Tsukuda
authors.forename: Tomoe
authors.initials: T
authors.lastname: Kusayanagi
authors.forename: Eri
authors.initials: E
authors.lastname: Umeda
authors.forename: Chihiro
authors.initials: C
authors.lastname: Watanabe
authors.forename: Yu-ta
authors.initials: YT
authors.lastname: Tosaki
authors.forename: Shinji
authors.initials: S
authors.lastname: Kamisuki
authors.forename: Toshifumi
authors.initials: T
authors.lastname: Takeuchi
authors.forename: Yoichi
authors.initials: Y
authors.lastname: Takakusagi
authors.forename: Isamu
authors.initials: I
authors.lastname: Shiina
authors.forename: Fumio
authors.initials: F
authors.lastname: Sugawara
mesh_terms: D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002352:Carrier Proteins / Q000737:chemistry / Q000378:metabolism*; D045744:Cell Line, Tumor; D061505:Cell Surface Display Techniques; D006801:Humans; D008969:Molecular Sequence Data; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism; D051057:Proto-Oncogene Proteins c-akt / Q000378:metabolism; D011759:Pyrrolidines / Q000494:pharmacology*; D015398:Signal Transduction / Q000187:drug effects; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D002352:Carrier Proteins; C478016:GIGYF2 protein, human; D011759:Pyrrolidines; C528171:ridaifen-B; D013629:Tamoxifen; D019869:Phosphatidylinositol 3-Kinases; D051057:Proto-Oncogene Proteins c-akt