発表者
渡部 拓 株式会社医学生物学研究所
タイトル
Fluoppi for evaluating plasma membrane penetration and activity of PPI modulators simultaneously.
要旨
Even successful PPI modulator is discovered by cell free methods, its penetration into living cells is often hampered by the plasma membrane. To provide a solution, we developed a very robust functional readout method called Fluoppi (Fluorescent Protein-Protein Interaction-visualization). The method allows visualization of the modulating effect of compounds on target PPIs inside living cells in single cell resolution. Fluoppi utilizes a simple output, where the distribution of fluorescence signal is either diffused (no protein-protein interaction) or foci patterned (protein-protein interactions present). It is easy and clear to monitor formation and/or degradation of the foci within the cell over time. This allows researchers quantify modulator effects, including PPI modulation durations- which can vary from several minutes to a few hours. In conclusion, Fluoppi is a powerful method applicable for hit identification to lead optimization phases in the drug discovery process.
