Targeting BIG3–PHB2 interaction to overcome tamoxifen resistance in breast cancer cells
Tetsuro Yoshimaru,Masato Komatsu,Taisuke Matsuo,Yi-An Chen,Yoichi Murakami,Yoichi Murakami,Kenji Mizuguchi,Eiichi Mizohata,Tsuyoshi Inoue,Miki Akiyama,Rui Yamaguchi,Seiya Imoto,Satoru Miyano,Yasuo Miyoshi,Mitsunori Sasa,Yusuke Nakamura,Yusuke Nakamura,Toyomasa Katagiri +17 more
TLDR
A cell-permeable peptide inhibitor, called ERAP, that regulates multiple ERα-signalling pathways associated with tamoxifen resistance in breast cancer cells by inhibiting the interaction between BIG3 and PHB2 is reported.Abstract:
Oestrogen receptor-α (ERα) signalling has a role in breast cancer drug resistance. Here, the authors report a synthetic peptide that disrupts the interaction between the signalling molecules BIG3 and PHB2, and thereby suppresses tamoxifen resistance.read more
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Xanthohumol suppresses oestrogen-signalling in breast cancer through the inhibition of BIG3-PHB2 interactions
Tetsuro Yoshimaru,Masato Komatsu,Etsu Tashiro,Masaya Imoto,Hiroyuki Osada,Yasuo Miyoshi,Junko Honda,Mitsunori Sasa,Toyomasa Katagiri +8 more
TL;DR: XN treatment effectively prevented the BIG3-PHB2 interaction, thereby releasing PHB2 to directly bind to both nuclear- and cytoplasmic ERα, leading to the complete suppression of the E2-signalling pathways and ERα-positive breast cancer cell growth both in vitro and in vivo.
References
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Journal ArticleDOI
Tamoxifen for Prevention of Breast Cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study
TL;DR: Tamoxifen decreases the incidence of invasive and noninvasive breast cancer and its use as a breast cancer preventive agent is appropriate in many women at increased risk for the disease.
Journal ArticleDOI
Cancer statistics, 2006.
Ahmedin Jemal,Rebecca L. Siegel,Elizabeth Ward,Taylor Murray,Jiaquan Xu,Carol Smigal,Michael J. Thun +6 more
TL;DR: The American Cancer Society estimated the number of new cancer cases and deaths expected in the United States in the current year and compiles the most recent data on cancer incidence, mortality, and survival based on incidence data from the National Cancer Institute and mortality data from National Center for Health Statistics as discussed by the authors.
Journal ArticleDOI
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.
Lyubomir T. Vassilev,Binh Thanh Vu,Bradford Graves,Daisy Carvajal,Frank John Podlaski,Zoran Filipovic,Norman Kong,Ursula Kammlott,Christine Lukacs,Christian Klein,Nader Fotouhi,Liu Emily Aijun +11 more
TL;DR: In this article, the authors identify potent and selective small-molecule antagonists of MDM2 and confirm their mode of action through the crystal structures of complexes, leading to cell cycle arrest, apoptosis, and growth inhibition of human tumor xenografts.
Journal ArticleDOI
The PSIPRED protein structure prediction server.
TL;DR: The PSIPRED protein structure prediction server allows users to submit a protein sequence, perform a prediction of their choice and receive the results of the prediction both textually via e-mail and graphically via the web.
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