| 摘要 |
Hydrolyzable prodrugs according to the present invention are activated by proteases located in the cell membranes of metastatic cells to yield active anticancer drugs that can be taken up by the metastatic cells. In general, a hydrolyzable prodrug according to the present invention comprises an amino-terminal capped peptide that is a substrate for a peptidohydrolase located on the surface of a metastatic cell covalently linked to a therapeutic drug through a self-immolating spacer of sufficient length to prevent the occurrence of steric hindrance. The therapeutic drug is typically an anticancer drug. The anticancer drug is typically doxorubicin, taxol, camptothecin, mitomycin C, or esperamycin. Typically, the peptidohydrolase that hydrolyses the substrate of the hydrolyzable prodrug is cathepsin B. |
