Establishment of high-throughput screening technology to accelerate transporter-targeted drug discovery

2023 Fiscal Year Final Research Report

• Project/Area Number: 21K19338
• Research Category: Grant-in-Aid for Challenging Research (Exploratory)
• Allocation Type: Multi-year Fund
• Review Section: Medium-sized Section 47:Pharmaceutical sciences and related fields
• Research Institution: Okayama University
• Principal Investigator: Miyaji Takaaki 岡山大学, 自然生命科学研究支援センター, 研究教授 (40550314)
• Project Period (FY): 2021-07-09 – 2024-03-31
• Keywords: トランスポーター / 創薬 / スクリーニング

Outline of Final Research Achievements

Because there was no optimal method to evaluate the transport activity, the function of majority of transporters remained unknown. In this study, we aimed to establish universal evaluation system of eukaryotic transporters to be suitable for identifying unknown functions and drug screening. We selected candidate proteins by organellar proteomics, and established over-expression and purification system of the transporters. Furthermore, we selected the candidates of transport substrate by biding screening, and identified transport function of transporters and the inhibitors by reconstituted proteoliposomes containing purified transporter. Thus, we have constructed a platform for function analysis and drug discovery of eukaryotic transporters using the over-expression and purification system.

Free Research Field

膜輸送分子生物学

Academic Significance and Societal Importance of the Research Achievements

トランスポーター標的型の医薬品は全体の約7％しかこれまでに上市されていないため、トランスポーター創薬は未開拓な研究領域の一つである。本研究技術によって、トランスポーターの機能同定から創薬研究までの方法を確立することができた。本研究技術は全てのタイプのトランスポーターを高感度に定量評価できるため、トランスポーター創薬研究のパラダイムシフトが期待される。