2014 Fiscal Year Final Research Report
Development of specific modulators for nuclear receptors and elucidation of their functions
| Project Area | Establishment of Integrative Multi-level Systems Biology and its Applications |
|---|
| Project/Area Number |
22136013
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research on Innovative Areas (Research in a proposed research area)
|
| Allocation Type | Single-year Grants |
|---|
| Review Section |
Complex systems
|
|---|
| Research Institution | Tokyo Medical and Dental University |
|---|
Principal Investigator |
|
|---|
| Co-Investigator(Renkei-kenkyūsha) |
HIRANO Tomoya 東京医科歯科大学, 生体材料工学研究所, 准教授 (20396980)
FUJII Shinya 東京医科歯科大学, 生体材料工学研究所, 助教 (60389179)
|
|---|
| Project Period (FY) |
2010-04-01 – 2015-03-31
|
| Keywords | 核内受容体 / 遺伝子転写制御 / 脂溶性ファーマコフォア / カルボラン / 高周期第１４族元素 / 蛍光性リガンド / 脂溶性ビタミン |
|---|
| Outline of Final Research Achievements |
Novel specific modulators of various nuclear receptors such as receptors for retinoids, vitamin D, and steroid hormones were developed, and their functions were elucidated. First, novel nuclear receptor ligands bearing a carborane or silyl-/germyl-containing substituents as the hydrophobic pharmacophore were developed. Second, the fluorescent ligands for steroid hormone receptors were synthesized, and their biological functions and fluorescent properties were elucidated. Third, novel derivatives of vitamin K as possible active metabolite were designed and synthesized. Furthermore, the strategies of the research on nuclear receptors were applied to the development of modulators of Store-Operated Calcium Entry (SOCE) and transcriptional cofactor, TAZ. These novel compounds of nuclear receptors and related molecules would be useful for the fundamental research on nuclear receptors and their clinical applications.
|
| Free Research Field |
医薬化学
|
