Approach to the novel molecular target of endocrine disrupter tamoxifen "endoplasmic reticulum membrane receptor"

2015 Fiscal Year Final Research Report

• Project/Area Number: 26550040
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Risk sciences of radiation and chemicals
• Research Institution: Kyushu University
• Principal Investigator: Shimohigashi Yasuyuki 九州大学, 理学(系)研究科(研究院), 教授 (00211293)
• Co-Investigator(Renkei-kenkyūsha): SUYAMA Keitaro 九州大学, 基幹教育院, 助教 (60707222)
• Project Period (FY): 2014-04-01 – 2016-03-31
• Keywords: 有害化学物質 / 内分泌かく乱物質 / タモキシフェン / 乳がん / 小胞体膜受容体

Outline of Final Research Achievements

The principal objective of this project is to identify a novel endoplasmic reticulum membrane receptor protein, to which tamoxifen, an anti-breast cancer drug, binds specifically, and also to develop a novel series of drug derivatives that do not bind to this tamoxifen receptor. We succeeded in narrowing down the candidate proteins, but with no isolation and purification. This tamoxifen receptor is present generally in mammalian cells. We further succeeded in the synthesis of compounds that bind to the estrogen receptor, but not to the tamoxifen receptor present in the endoplasmic reticulum membrane. These compounds were found to function as antiestrogen drugs, exhibiting the suppression action for0 breast cancer cell multiplication.

Free Research Field

環境生化学、化学物質影響科学、受容体科学