| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2015: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| 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.
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