Development of molecular probes for steroid hormone receptor functions

2014 Fiscal Year Final Research Report

• Project/Area Number: 24590137
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Ochanomizu University
• Principal Investigator: TANATANI Aya お茶の水女子大学, 大学院人間文化創成科学研究科, 准教授 (40361654)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: ステロイドホルモン / 核内受容体 / アンドロゲン / プロゲステロン / アンタゴニスト / 蛍光性リガンド / クマリン

Outline of Final Research Achievements

In this study, the specific ligands and fluorescence probes for steroid hormone nuclear receptors were developed.
(1) Phthalazinone derivatives were developed as novel androgen antagonists, and acted as antagonists towards both wild-type and mutated ARs. As progesterone antagonists, compounds bearing a carborane or adamantane as the hydrophobic pharmacophore were developed.
(2) Coumarine derivatives were developed as fluorescent progesterone antagonists, whose fluorescence intensity was strongly increased by binding to progesterone receptor. Coumarine derivatives with androgen antagonistic activity were also developed.

Free Research Field

医薬化学