Development of novel nuclear receptor modulators based on the chemical posttranslational modifications

2017 Fiscal Year Final Research Report

• Project/Area Number: 16K15138
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Drug development chemistry
• Research Institution: The University of Tokyo
• Principal Investigator: Fujii Shinya 東京大学, 分子細胞生物学研究所, 講師 (60389179)
• Research Collaborator: NUMADATE Akiyoshi
• Project Period (FY): 2016-04-01 – 2018-03-31
• Keywords: 転写因子 / 核内受容体 / アンドロゲン受容体 / 化学的翻訳後修飾

Outline of Final Research Achievements

Nuclear receptors, ligand-dependent transcription factors, are promising targets of drug discovery. Recent studies have revealed various physiological functions of nuclear receptors which are not able to be modulated by the conventional ligands. In this study, development of new type of nuclear receptor modulators bearing novel mechanism of action have been investigated.
Focusing on the diphenylmethane derivative which was reported to bind the N-terminal domain of nuclear androgen receptor covalently, structural development studies were investigated. As a result, compounds exerting transcription inducing or repressing activity were obtained.

Free Research Field

創薬化学