Enzyme transformation to modulate the ligand-receptor interactions between small molecules.

Enzymatic transformation is a fundamental process to control ligand-receptor interactions among proteins for signal transduction in cells. Here we report the first example of enzymatic transformation regulated ligand-receptor interactions of small molecules, in which enzymatic reaction changes the stoichiometry of the ligand-receptor binding from 1 : 1 to 1 : 2. We also show that this unique integration of enzymatic transformation and ligand-receptor interactions of small molecules is able to affect the fate of cells.