Discovery of ubiquitin-activating enzyme inhibitors designed based on its catalytic mechanism
| Project/Area Number |
26870495
|
|---|
| Research Category |
Grant-in-Aid for Young Scientists (B)
|
| Allocation Type | Multi-year Fund |
|---|
| Research Field |
Chemical pharmacy
Drug development chemistry
|
|---|
| Research Institution | Kyoto Prefectural University of Medicine |
|---|
Principal Investigator |
Itoh Yukihiro 京都府立医科大学, 医学(系)研究科(研究院), 講師 (30636402)
|
|---|
| Project Period (FY) |
2014-04-01 – 2017-03-31
|
| Project Status |
Completed (Fiscal Year 2016)
|
| Budget Amount *help |
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2016: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2015: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
|
|---|
| Keywords | ドラッグデザイン / 低分子薬物 / 触媒メカニズム / 創薬化学 / ケミカルバイオロジー |
|---|
| Outline of Final Research Achievements |
It has been reported that ubiquitin-activating enzyme is highly expressed in leukemic cells and that inhibition of the enzyme disturbs their proliferation.
Therefore, ubiquitin-activating enzymes are interesting as a drug target. In this study, we attempted to discover ubiquitin-activating enzyme inhibitors. Based on the catalytic mechanism of ubiquitin-activating enzyme, we designed and synthesized several compounds which were expected to show inhibitory activity dependent on enzyme reaction. As a result of their biological evaluation, we succeeded in identification of a compound inhibiting ubiquitin-activing enzyme.
|
Report
(4 results)
Research Products
(3 results)
