Development of GSTP1 fluorescent probes for the elucidation of the function of GSTP1 in cancer cells.

2021 Fiscal Year Final Research Report

• Project/Area Number: 18K05362
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 37030:Chemical biology-related
• Research Institution: Tokyo University of Pharmacy and Life Science
• Principal Investigator: Yuuta Fujikawa 東京薬科大学, 生命科学部, 准教授 (90645144)
• Project Period (FY): 2018-04-01 – 2022-03-31
• Keywords: 蛍光プローブ / GST / グルタチオン / レドックス

Outline of Final Research Achievements

In this study, we developed fluorescent probes with different properties targeting GSTP1. We developed a probe, Ps-TG3, which can be applied to cultured cells without prodrugation, which was required for existing fluorescent probes, and succeeded in live cell imaging. We also succeeded in developing a red-orange GSTP1 fluorescent probe, Ps-CF, which can be used in combination with a green fluorescent probe targeting GGT, another cancer marker enzyme, to enable simultaneous detection of GSTP1 and GGT activity. Since these results enable the simultaneous detection of multiple cancer marker enzymes, including GSTP1, it is considered important findings for the detection of small tumors and clarification of the mechanism of GSTP1.

Free Research Field

ケミカルバイオロジー

Academic Significance and Societal Importance of the Research Achievements

本研究により、がんで高発現している薬物代謝酵素GSTP1を標的とした、物理化学的特性や蛍光特性の異なる複数種類の蛍光プローブを開発することに成功した。これらの蛍光プローブは、微小がんの検出やGSTP1の機能解析のための有用なツールとなり得る。ただし、より汎用性の高いプローブを得るには、プローブの特性に改善の余地があることから、さらなる構造最適化なども検討する必要がある。