作者:Annastasiah Mhaka、Sam R Denmeade、Wei Yao、John T Isaacs、Saeed R Khan
DOI:10.1016/s0960-894x(02)00433-x
日期:2002.9
A method for targeted delivery of the cytotoxic agent 5-fluorodeoxyuridine (FudR) (1) to sites of metastatic prostate cancer is described. The prodrug was synthesized by coupling the active drug (FudR) to the PSA-peptide via a self-cleaving diamino acid linker to produce HSSKLQ-Leu-Aib-FudR. This prodrug serves as a substrate for prostate specific antigen (PSA). This approach permitted efficient conversion of the inactive prodrug back to the active cytotoxic state by the enzymatic activity of PSA which is highly expressed by prostate cells. (C) 2002 Elsevier Science Ltd. All rights reserved.