| 研究実績の概要 |
Due to delays in gaining access to cell-lines stably over-expressing the target bio-synthetic enzymes and thus in accessing purified target enzymes the planned in vitro assay series has been slightly delayed (see blow). In the meantime, the prepared reference material was used to probe receptor specificity in ex vivo assay systems, such as neuronal ex-plants. Additionally, a homology model of the target G-coupled protein receptor has been developed and is now ready for validation. Utilizing the established synthetic route via P(III) towards the target lipids, a novel, switch-able, fluorescent lipid analogue has been developed and its application for in vitro assay systems has been established. Publication of these results has been accepted in the Journal Scientific Reports.
|
| 今後の研究の推進方策 |
The homology model established during the last fiscal year will be validated against the experimental ex vivo results of PtdGlc analogues utilizing molecular dynamics simulations of the receptor and synthetic agonist/antagonist in a membrane environment. This will allow to develop a structure activity map and provide the basis for the next publication. Experimentally, after gaining access to sufficient purified target enzyme, the in vitro assays will be performed as planned.
|
