2015 Fiscal Year Final Research Report
Lysophosphatidic acid receptor 4 as a potential drug target for the treatment of type 2 diabetes
Project/Area Number |
26860169
|
Research Category |
Grant-in-Aid for Young Scientists (B)
|
Allocation Type | Multi-year Fund |
Research Field |
General pharmacology
|
Research Institution | Akita University |
Principal Investigator |
Ohto-N Takayo 秋田大学, 医学(系)研究科(研究院), 助教 (80511378)
|
Project Period (FY) |
2014-04-01 – 2016-03-31
|
Keywords | リゾホスファチジン酸 |
Outline of Final Research Achievements |
Lysophosphatidic acid receptor 4 (LPA4)-deficient mice are resistant to high-fat diet-induced diabetes. This observation suggests that LPA4 antagonists may provide new therapeutic approaches for type 2 diabetes. Thus, the purpose of this project was to find LPA4 antagonists by screening a chemical library of Drug Discovery Initiative, The University of Tokyo. I used rat neuroblastoma B103 cells, which lack endogenous responses to LPA, to assess the functions of LPA4. In contrast to the parental B103 cells, LPA4-expressing B103 cells (B103-LPA4) showed Ca2+ influx in response to LPA. By using B103-LPA4 cells, I identified 37 compounds that activate LPA4 predominantly. Furthermore, I examined commercially available two compounds, which were reported to be LPA4 antagonists, and their derivatives. However, no antagonist activities were detected in these compounds.
|
Free Research Field |
脂質生物学
|