abstract |
Covalent complexation of the alpha amino acid ester to the modulator of the target intracellular enzyme or receptor activity, wherein the ester group of the complex is hydrolysable to the corresponding acid by one or more intracellular carboxylesterase enzymes, It leads to the accumulation of carboxylic acid hydrolysates within the cell, allowing improved or more extended enzyme or receptor modification compared to unconjugated modulators. [Selection] Figure 2 |