Selective Cell Targeting by High and Low Affinity Ligands on Cell Surface

2017 Fiscal Year Final Research Report

• Project/Area Number: 16K13104
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Chemical biology
• Research Institution: Institute of Physical and Chemical Research
• Principal Investigator: TANAKA Katsunori 国立研究開発法人理化学研究所, 田中生体機能合成化学研究室, 主任研究員 (00403098)
• Project Period (FY): 2016-04-01 – 2018-03-31
• Keywords: 生体分子 / 糖鎖 / 細胞 / 認識 / 有機化学

Outline of Final Research Achievements

In the field of molecular imaging, the target selectivity is one of the most important factors in determining the degree of imaging contrast. We developed an entirely unexplored idea that is based on a pre-targeting strategy by a) simultaneously recognizing two receptors using high- and low-affinity ligands and b) ligating them directly on the target cell surface. Glycan ligands with fluorescent label bound to the cell surface, even with mM binding affinity levels, can be tightly anchored by the pre-targeted high-affinity peptide ligand on the cell surface. The advantage of using low-affinity glycan ligands is that excess of the labeled glycans can be washed off from the cells. Through this approach, unspecific fluorescence background can be minimized. In this work, we demonstrated this strategy to differentiate various cancer cell lines by utilizing peptide and various different glycan structures.

Free Research Field

有機合成化学、グライコケミカルバイオロジー